Autophagy

Autophagy製品

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S1078 MK-2206 2HCl MK-2206 2HCl は高い選択性をもつ Akt1/2/3 阻害剤であり、cell-free assay における IC50 はそれぞれ 8 nM/ 12 nM/ 65 nM です。一方で、他の250種におよぶキナーゼ (kinases) に対しては活性が検出されていません。MK-2206 2HCl はがん細胞におけるオートファジー (autophagy) アポトーシス (apoptosis) に関与します。臨床第2相試験中
Nat Commun, 2024, 15(1):686
Cell Rep Med, 2024, 5(2):101420
Int J Biol Sci, 2024, 20(4):1389-1409
S1039 Rapamycin (Sirolimus) ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。
Drug Resist Updat, 2024, 73:101063
Cell Rep Med, 2024, 5(2):101420
J Adv Res, 2024, S2090-1232(24)00079-1
S1105 LY294002 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
Cell Rep Med, 2024, 5(2):101420
Biomed Pharmacother, 2024, 172:116259
Stem Cell Reports, 2024, 19(2):196-210
S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
Cell, 2024, 187(4):945-961.e18
Nat Commun, 2024, 15(1):866
Cell Rep Med, 2024, 5(2):101396
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1049 Y-27632 2HCl Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):827
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
S2767 3-MA (3-Methyladenine) 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared.
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1669
Cancer Lett, 2024, 586:216695
S1263 Laduviglusib (CHIR-99021) ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S1120 Everolimus エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。
Cell, 2024, 187(3):712-732.e38
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
Cell Death Dis, 2024, 15(1):31
Cell Mol Life Sci, 2024, 81(1):59
mBio, 2024, e0313623.
S1025 Gefitinib Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Gastroenterology, 2024, S0016-5085(24)00062-3
Phytomedicine, 2024, 125:155351
mBio, 2024, e0228723.
S1166 Cisplatin シスプラチン (Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)) は無機白金錯体であり、腫瘍細胞中において DNA 付加物を形成することにより DNA 合成を阻害する能力を有します。シスプラチンはフェロトーシス (ferroptosis) を活性化し、オートファジー (autophagy) を誘導します。溶液は都度調製してください。DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.Solutions are unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):866
Clin Cancer Res, 2024, 30(1):187-197
Cancer Lett, 2024, 586:216695
S1267 Vemurafenib (PLX4032) Vemurafenib (RG7204, RO5185426,PLX4032) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Biochem Pharmacol, 2024, 219:115952
Nat Cancer, 2023, 4(2):240-256
Nat Commun, 2023, 14(1):3251
S2924 Laduviglusib (CHIR-99021) HCl ラドゥビグルシブ塩酸塩 (Laduviglusib (CHIR-99021; CT99021) HCl) は CHIR-99021 の塩酸塩で、GSK-3α/β 阻害剤 (IC50 = 10 nM/6.7 nM) です。 CHIR-99021 は、最も近縁なホモログである Cdc2 および ERK2 と比較して、GSK-3 に対して 500 倍を超える選択性を示します。 CHIR-99021 は、Wnt/β-カテニン シグナル伝達経路の強力な薬理学的活性化因子です。 CHIR-99021 は、光誘発されるオートファジー (autophagy) を大幅にレスキューし、GR、RORα、およびオートファジー関連タンパク質量を増大します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
S1378 Ruxolitinib ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
Acta Neuropathol, 2024, 147(1):28
Theranostics, 2024, 14(3):1224-1240
Cell Rep, 2024, 43(2):113600.
S1023 Erlotinib HCl Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Nat Commun, 2023, 14(1):1559
Nat Commun, 2023, 14(1):7863
Cell Rep, 2023, 42(8):112868
S7786 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
NPJ Precis Oncol, 2024, 8(1):3
Transl Oncol, 2024, 39:101834
J Biol Chem, 2024, S0021-9258(24)00139-X
S8048 Venetoclax (ABT-199) Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
Nat Commun, 2024, 15(1):1821
Cell Death Dis, 2024, 15(2):131
Cell Death Discov, 2024, 10(1):35
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Clin Epigenetics, 2024, 16(1):13
S1021 Dasatinib Dasatinibは新規の強力なマルチターゲット阻害剤であり、cell-free assy における Abl, Src および c-Kit に対する IC50 はそれぞれ < 1 nM, 0.8 nM および 79 nM です。Dsatinib はオートファジー (autophagy)アポトーシス (apoptosis) を誘発し、抗腫瘍活性を示します。
Nature, 2024, 10.1038/s41586-024-07079-8
Cell Rep Med, 2024, 5(2):101416
Cell Rep Med, 2024, 5(2):101412
S1250 Enzalutamide エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。
Cancers (Basel), 2024, 16(2)296
bioRxiv, 2024, 10.1101/2024.01.16.575611
bioRxiv, 2024, 10.1101/2023.12.01.569685
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Adv Sci (Weinh), 2024, 11(4):e2304987
Genome Biol, 2024, 25(1):58
Cell Death Discov, 2024, 10(1):95
S2111 Lapatinib Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Drug Resist Updat, 2024, 73:101066
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 10.1038/s41467-023-39059-3
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):5242
J Clin Invest, 2023, 133(18)e168352
S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S7840 Dorsomorphin Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
iScience, 2024, 27(2):108852
J Ethnopharmacol, 2024, 324:117814
J Cell Mol Med, 2024, 28(2):e18055
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
NPJ Precis Oncol, 2024, 8(1):52
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Cancer Res Commun, 2024, 4(2):349-364
S1150 Paclitaxel パクリタキセル (Paclitaxel (NSC 125973, PTX)) は微小管を安定化することで脱重合を阻害します。ヒト血管内皮細胞における IC50 は 0.1 pM です。
Adv Sci (Weinh), 2024, 11(5):e2305035
Cell Death Differ, 2024, 10.1038/s41418-024-01267-9
Clin Transl Med, 2024, 14(2):e1567
S1413 Bafilomycin A1 (Baf-A1) バフィロマイシン A1 (Bafilomycin A1(Baf-A1)) は液胞 H+-ATPase 阻害剤で、IC50 は 0.44 nM です。 バフィロマイシン A1 は、オートファジー (autophagy) を阻害する一方で、アポトーシス (apoptosis) を誘導することがわかっています。
Nature, 2024, 626(8000):874-880
Nat Commun, 2024, 15(1):631
Nat Commun, 2024, 15(1):1669
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Cell Rep, 2024, 43(1):113575
Int J Mol Sci, 2024, 25(2)1278
Cancer Res Commun, 2024, 4(2):349-364
S1011 Afatinib アファチニブ (Afatinib) は in vitro において EGFR/ErbB を不可逆的に阻害します。IC50 は EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4) に対してそれぞれ 0.5, 0.4, 10, 14 および 1 nM です。アファチニブによってオートファジー (autophagy) が誘発されることが報告されています。
Cell, 2024, 187(3):712-732.e38
Cell Rep, 2024, 43(1):113614
NPJ Precis Oncol, 2024, 8(1):3
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Gastroenterology, 2024, S0016-5085(24)00062-3
bioRxiv, 2024, 2024.01.29.577409
Cell Discov, 2023, 9(1):47
S2215 DAPT DAPT (GSI-IX、LY-374973) は新規の γ-セクレターゼ 阻害剤であり、HEK 293 細胞で 20 nM の IC50 で Aβ 産生を阻害します。 DAPT はヒト舌癌細胞のアポトーシス(apoptosis) を促進し、オートファジー (autophagy) を調節します。
Genome Biol, 2024, 25(1):58
Br J Cancer, 2024, 10.1038/s41416-024-02576-z
Antibodies (Basel), 2024, 13(1)15
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Sci Rep, 2024, 14(1):4303
bioRxiv, 2024, 2024.01.17.575938
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):830
Nat Commun, 2024, 15(1):1041
S1092 KU-55933 KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Nat Commun, 2024, 15(1):1300
Nat Cancer, 2023, 4(2):240-256
Cancer Res, 2023, 83(1):141-157
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575847
Cancer Discov, 2023, 13(7):1696-1719
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cell Commun Signal, 2023, 21(1):342
Phytomedicine, 2023, 117:154918
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Nature, 2023, 621(7978):415-422
Circulation, 2023, 148(19):1459-1478
Nat Commun, 2023, 14(1):6088
S2226 Idelalisib (CAL-101) Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Transl Oncol, 2024, 43:101857
Cancer Cell, 2023, 41(6):1103-1117.e12
Nat Cancer, 2023, 4(10):1508-1525
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
J Biol Chem, 2024, S0021-9258(24)00057-7
Nat Neurosci, 2023, none
S1714 Gemcitabine Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2024, 15(1):1287
Genes Dis, 2024, 11(1):430-448
iScience, 2024, 27(1):108667
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.04.574149
Cell Rep Med, 2023, 4(5):101025
Blood Cancer J, 2023, 13(1):42
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Cell Death Discov, 2024, 10(1):74
EMBO Mol Med, 2023, e16235.
Cell Syst, 2023, S2405-4712(23)00116-3
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Antioxidants (Basel), 2024, 13(1)114
Heliyon, 2024, 10(1):e23426
J Cancer, 2024, 15(3):685-698
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
Mol Neurodegener, 2023, 18(1):67
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Int J Chron Obstruct Pulmon Dis, 2024, 19:269-279
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
S1224 Oxaliplatin Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Mol Cancer, 2024, 23(1):23
Gastroenterology, 2024, S0016-5085(24)00062-3
NPJ Precis Oncol, 2024, 8(1):52
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Clin Cancer Res, 2023, 29(16):3151-3161
Cell Death Dis, 2023, 14(7):463
S1178 Regorafenib Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S1237 TMZ(Temozolomide) テモゾロミド (Temozolomide (NSC 362856,TMZ,CCRG 81045,Methazolastone)) はDNA 環上の窒素原子と環外酸素を修飾することが可能な単官能性 SN1 アルキル化剤であり、中間体である MTIC を経て、活性代謝産物であるメチルジアゾニウムカチオン (methyl diazoniumcation) に分解されると、生理学的 pH において DNA にメチル基を転移します。テモゾロミドはアポトーシス (apoptosis) を誘発し、抗がん活性を呈します。L-1210 細胞および L-1210/BCNU 細胞における DNA 損傷誘導剤です。
Cancer Cell Int, 2024, 24(1):36
bioRxiv, 2024, 2024.01.20.576487.
Research Square, 2024, 10.21203/rs.3.rs-3886648/v1
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Adv Sci (Weinh), 2023, 10(25):e2301753
Cell Rep Med, 2023, 4(12):101339
Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120
S1129 SRT1720 HCl SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.21.576539
Chinese Journal of Tissue Engineering Research, 2024, (28): 4447-4454.
Small, 2023, e2300584.
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Cell Rep Med, 2024, 5(2):101396
Theranostics, 2024, 14(4):1561-1582
Clin Transl Med, 2024, 14(2):e1583
S1149 Gemcitabine HCl ゲムシタビン塩酸塩 (Gemcitabine (LY-188011, NSC 613327) HCl) は DNA 合成阻害剤であり、 PANC1 細胞、 MIAPaCa2 細胞、 BxPC3 細胞および Capan2 細胞における IC50 はそれぞれ 50 nM, 40 nM, 18nM, 12 nM です。
Int J Biol Sci, 2024, 20(4):1389-1409
Phytomedicine, 2024, 155377
Neoplasia, 2024, 47:100951
S7810 Afatinib Dimaleate Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
J Invest Dermatol, 2024, S0022-202X(23)03210-4
RSC Adv, 2023, 13(16):11037-11043
Biochem Biophys Rep, 2023, 34:101436
S1582 H 89 2HCl H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
S1191 Fulvestrant フルベストラント (Fulvestrant (ICI-182780, ZD 9238, ZM 182780)) はエストロゲン受容体 (estrogen receptor, ER) アンタゴニストであり、cell-free assay における IC50 は 0.94 nM です。フルベストラントはまたオートファジー (autophagy)アポトーシス (apoptosis) を誘導し、抗腫瘍活性を呈します。
Cancers (Basel), 2024, 16(3)678
Cancers (Basel), 2024, 16(2)257
bioRxiv, 2024, 10.1101/2024.01.16.575899
S2449 Forskolin (Colforsin) コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXRFXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。
iScience, 2024, 27(2):108857
bioRxiv, 2024, 2024.01.15.574730
Cell Stem Cell, 2023, 30(7):938-949.e7
S1033 Nilotinib Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):651
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
NPJ Precis Oncol, 2023, 7(1):132
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Signal Transduct Target Ther, 2023, 8(1):183
Nucleic Acids Res, 2023, 51(9):4451-4466
Autophagy, 2023, 10.1080/15548627.2023.2281128
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Cell Death Dis, 2024, 15(1):35
Sci Adv, 2024, 10(8):eadk3663
Signal Transduct Target Ther, 2023, 8(1):229
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Neoplasia, 2024, 48:100966
Nat Commun, 2023, 14(1):6505
S1786 Verteporfin ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。 また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。 ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。
Bone Res, 2024, 12(1):12
Cancer Lett, 2024, 587:216692
iScience, 2024, 27(3):109125
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Int J Mol Sci, 2024, 25(2)959
Mol Cancer, 2023, 22(1):66
Cells, 2023, 12(12)1624
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nat Commun, 2024, 15(1):35
Elife, 2024, 13e80684
Nat Genet, 2023, 55(10):1721-1734
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Cell Death Dis, 2023, 14(10):672
iScience, 2023, 26(7):107090
Int J Mol Sci, 2023, 24(20)15258
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
S1241 Vincristine sulfate Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
iScience, 2024, 27(1):108667
Cell Rep Med, 2023, 4(12):101339
Acta Neuropathol Commun, 2023, 11(1):6
S1057 Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Emerg Microbes Infect, 2022, 1-29
Cancers (Basel), 2022, 14(22)5602
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Nat Cancer, 2023, 4(9):1345-1361
Cell Reports, 2023, 112328
Cell Rep, 2023, 42(4):112328
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
Nat Commun, 2023, 14(1):5051
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Nat Commun, 2024, 15(1):1750
Cell Rep Med, 2024, 5(2):101416
Biochem Pharmacol, 2024, S0006-2952(24)00048-0
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S2775 Nocodazole Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Life Sci Alliance, 2024, 7(4)e202302257
Nat Metab, 2023, 5(2):277-293
Adv Sci (Weinh), 2023, 10(7):e2205566
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
PLoS Pathog, 2024, 20(1):e1011958
Kidney Int, 2023, 104(5):943-955
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
Mol Cancer, 2023, 22(1):204
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Nat Commun, 2023, 14(1):390
Aging Cell, 2023, e13888.
BMC Cancer, 2023, 23(1):499
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Cell Rep, 2024, 43(1):113575
Clin Epigenetics, 2023, 15(1):19
Transl Oncol, 2023, 39:101779
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Comput Struct Biotechnol J, 2023, 21:1157-1168
Mol Cell Biol, 2023, 43(1):1-21
J Cell Commun Signal, 2023, 17(3):975-989
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Cell Commun Signal, 2024, 22(1):117
Mol Carcinog, 2024, 63(3):430-447
Research Square, 2024, 10.21203/rs.3.rs-3834927/v1
S1322 Dexamethasone Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Oncogene, 2024, 43(4):235-247
bioRxiv, 2024, 2024.01.29.577409
S8075 GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Acta Pharm Sin B, 2023, 13(6):2601-2612
Cell Death Dis, 2023, 14(7):461
Cell Death Dis, 2023, 14(12):830
S1075 SB216763 SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
Cell Death Dis, 2023, 14(8):500
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
PLoS One, 2024, 19(1):e0295629
Cancer Res Commun, 2024, 4(2):349-364
J Cell Biol, 2023, 222(2)e202205092
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Nat Commun, 2023, 14(1):3928
Cell Commun Signal, 2023, 21(1):25
JCI Insight, 2023, 8(14)e157027
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Clin Respir J, 2024, 18(1):e13731
Cell Death Dis, 2023, 14(7):469
Cell Death Dis, 2023, 14(7):469
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Gastroenterology, 2024, S0016-5085(24)00062-3
Oncologist, 2024, 29(1):15-24
Cell Rep Med, 2023, 4(4):101002
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
S7655 Telaglenastat (CB-839) CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
Signal Transduct Target Ther, 2023, 8(1):159
Cancer Discov, 2023, 13(7):1696-1719
J Thorac Oncol, 2023, S1556-0864(23)00197-1
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
bioRxiv, 2024, 2024.02.06.579216
Nat Commun, 2023, 14(1):6088
Nat Commun, 2023, 14(1):4991
S1648 Cytarabine Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Int J Mol Sci, 2024, 25(1)646
Cell Signal, 2024, 114:111004
S7307 GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Exp Mol Med, 2024, 56(2):408-421.
Cell Discov, 2023, 9(1):7
Cell Death Dis, 2023, 14(7):467
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines.
Cell Death Dis, 2023, 14(4):234
JCI Insight, 2023, 8(23)e164968
Phytomedicine, 2023, 115:154809
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
PLoS One, 2024, 19(1):e0295629
bioRxiv, 2024, 2024.01.20.576487.
Mol Cell, 2023, 83(13):2206-2221.e11
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Iran J Basic Med Sci, 2024, 27(3):360-365.
J Radiat Res, 2024, rrad107
Research Square, 2024, 10.21203/rs.3.rs-3872267/v1
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S5742 Deferoxamine mesylate Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115889
J Cancer, 2024, 15(3):685-698
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Cell Oncol (Dordr), 2023, 46(2):391-407
Biochem Pharmacol, 2023, 214:115681
Int J Mol Sci, 2023, 24(9)8037
S2180 Ixazomib (MLN2238) Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
iScience, 2023, 26(8):107302
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
NPJ Precis Oncol, 2024, 8(1):52
Cancer Discov, 2023, 13(10):2192-2211
Cancer Discov, 2023, 13(10):2192-2211
S8964 Actinomycin D (Dactinomycin) Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
Cell Mol Life Sci, 2024, 81(1):92
NPJ Precis Oncol, 2024, 8(1):22
Signal Transduct Target Ther, 2023, 8(1):63
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Acta Biomater, 2024, S1742-7061(24)00036-9
Int J Biol Sci, 2024, 20(2):784-800
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S7046 Brefeldin A (BFA) Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
Nat Commun, 2024, 15(1):203
Commun Biol, 2024, 7(1):161
Cancer Immunol Immunother, 2024, 73(1):7
S2285 Cryptotanshinone (Tanshinone C) Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
J Med Virol, 2023, 95(11):e29230
Microbiol Spectr, 2023, e0493222.
Evid Based Complement Alternat Med, 2023, 2023:1307323
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
S1792 Simvastatin Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
Cell Death Dis, 2023, 14(4):234
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Nat Commun, 2023, 14(1):6246
Nat Commun, 2023, 14(1):6246
Endocrinology, 2023, 164(6)bqad073
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HClcompetes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
J Exp Clin Cancer Res, 2023, 42(1):8
Cell Death Dis, 2023, 14(10):652
Cell Death Dis, 2023, 14(10):652
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Nat Commun, 2023, 14(1):1413
Nature Communications, 2023, 1413-2023)
Cancers (Basel), 2023, 15(3)610
S2843 BI-D1870 BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
BMC Cancer, 2024, 24(1):233
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
S2163 PF-4708671 PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.
Adv Sci (Weinh), 2023, 10(3):e2203718
Nucleic Acids Res, 2023, 51(22):12076-12091
CNS Neurosci Ther, 2023, 10.1111/cns.14475
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
J Immunother Cancer, 2023, 11(11)e007736
Clin Transl Med, 2023, 13(12):e1502
J Neuroinflammation, 2023, 20(1):168
S7130 PR-619 PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.
Nat Commun, 2024, 15(1):1642
J Nanobiotechnology, 2023, 21(1):117
Ecotoxicol Environ Saf, 2023, 263:115197
S8047 Dynasore Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).
Immunity, 2024, 57(2):287-302.e12
Nat Commun, 2024, 15(1):1669
J Exp Med, 2023, 220(3)e20221316
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Sci Adv, 2023, 9(28):eadf4766
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Cancers (Basel), 2024, 16(2)296
Biomedicines, 2024, 12(1)181
J Exp Clin Cancer Res, 2023, 42(1):204
S2061 Lovastatin Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). Lovastatin triggers autophagy.
DNA Repair (Amst), 2024, 134:103627
bioRxiv, 2024, 10.1101/2024.01.16.575899
Signal Transduct Target Ther, 2023, 8(1):183
S1590 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.
Sci Rep, 2024, 14(1):5038
Stem Cells Transl Med, 2023, szad085
J Nanobiotechnology, 2022, 20(1):148
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.
Mol Cell, 2023, 83(13):2206-2221.e11
J Transl Med, 2023, 21(1):115
Biochem Pharmacol, 2023, 214:115681
S3042 Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Nat Commun, 2024, 15(1):987
Neural Regen Res, 2024, 19(1):205-211
Regen Ther, 2024, 25:229-237
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Cell Rep, 2023, 42(8):112925
bioRxiv, 2023, 2023.01.17.524444
S7423 KN-93 Phosphate KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration.
PLoS Pathog, 2023, 19(3):e1011295
Ren Fail, 2023, 45(1):2172961
Nat Commun, 2022, 13-1:6117
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
Adv Skin Wound Care, 2023, 36(5):249-258
S7998 Entrectinib Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Biomolecules, 2023, 13(3)438
S3030 Niclosamide Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
Int J Nanomedicine, 2023, 18:7505-7521
Front Cell Dev Biol, 2023, 11:1062229
J Am Heart Assoc, 2023, 12(1):e027222
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Redox Biol, 2024, 70:103072
J Exp Clin Cancer Res, 2023, 42(1):236
J Exp Clin Cancer Res, 2023, 42(1):236
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.
Mol Cancer, 2023, 22(1):64
Int J Mol Sci, 2023, 24(6)5464
Molecules, 2022, 27(19)6149
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
Biomedicines, 2023, 10.3390/biomedicines11030759
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Dev Cell, 2023, 58(6):506-521.e5
Cell Death Dis, 2023, 14(9):627
Cell Death Dis, 2023, 14(9):627
S1135 Pemetrexed disodium Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cancer Cell, 2022, 40(10):1128-1144.e8
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Nat Commun, 2023, 14(1):2132
Redox Biol, 2023, 65:102833
Cell Rep, 2023, 42(2):112023
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Nucleic Acids Res, 2023, gkad796
Redox Biol, 2023, 66:102858
EMBO J, 2023, 42(20):e113743
S7751 VER155008 VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Signal Transduct Target Ther, 2023, 8(1):229
Mol Cell, 2023, 83(15):2810-2828.e6
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Neural Regen Res, 2024, 19(1):205-211
iScience, 2024, 27(3):109166
Commun Biol, 2023, 6(1):824
S1896 Hydroxyurea Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
bioRxiv, 2024, 10.1101/2024.01.04.574133
Cell Rep, 2023, 42(7):112660
Cell Rep, 2023, 42(10):113176
S7888 Spautin-1 Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.
J Adv Res, 2024, S2090-1232(24)00025-0
Mol Cancer, 2023, 22(1):204
Nat Commun, 2023, 14(1):2691
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
S4505 Vinblastine sulfate Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
J Immunother Cancer, 2023, 11(8)e007253
J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
Cell Rep, 2023, 42(4):112324
S4269 Vinorelbine ditartrate Vinorelbine ditartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cell Rep, 2023, 42(10):113176
J Pathol, 2023, 261(3):256-268
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00786-w
S1235 Letrozole Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy.
Mol Oncol, 2023, 10.1002/1878-0261.13541
Commun Biol, 2023, 6(1):695
Nature Communications, 2022, 13, 5258
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1.
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
Sci Rep, 2022, 12(1):6345
S7104 AZD1208 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Angiogenesis, 2024, 10.1007/s10456-024-09906-y
Mol Cancer, 2023, 22(1):64
Cell Rep, 2023, S2211-1247(23)00893-8
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
Cell Rep, 2024, 43(1):113575
PLoS Pathog, 2024, 20(1):e1011958
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Life Sci Alliance, 2023, 6(5)e202201605
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Commun, 2022, 13(1):6589
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
J Pers Med, 2022, 12(2)258
S8222 AS1842856 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
Cell Death Dis, 2023, 14(1):47
Cell Rep, 2023, 42(3):112186
Antioxidants -Basel), 2023, 12(10)1881
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Int J Mol Sci, 2023, 24(18)13830
ACS Cent Sci, 2022, 8(5):636-655
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
Transl Psychiatry, 2022, 12(1):130
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
Nat Commun, 2022, 13(1):2500
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
Nat Commun, 2023, 14(1):886
Environ Pollut, 2023, 323:121306
Exp Gerontol, 2023, 173:112091
S1204 Melatonin Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Ecotoxicol Environ Saf, 2023, 255:114719
Microbiol Res, 2023, 276:127480
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00875-w
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Nat Commun, 2024, 15(1):668
Cell Mol Life Sci, 2024, 81(1):92
Cell Death Discov, 2024, 10(1):95
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Nat Commun, 2024, 15(1):1277
Sci Rep, 2024, 14(1):4000
Drug Resist Updat, 2023, 70:100985
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
Sci Rep, 2022, 12(1):10616
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
bioRxiv, 2024, 10.1101/2024.01.22.575998
Nat Cell Biol, 2023, 25(7):975-988
Mol Cell, 2023, 83(19):3485-3501.e11
S2782 GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
Nat Commun, 2023, 14(1):2656
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
J Clin Invest, 2023, 133(18)e166490
J Clin Invest, 2023, 133(18)e166490
Aging Cell, 2023, 22(6):e13840
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Acta Pharm Sin B, 2023, 13(6):2601-2612
J Exp Clin Cancer Res, 2023, 42(1):320
Pharmacol Res, 2022, 177:106122
S7177 PF-543 hydrochloride PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
J Transl Med, 2024, 22(1):43
Int J Mol Sci, 2023, 24(9)8303
Cell Res, 2022, 10.1038/s41422-022-00614-0
S7289 PFK15 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
Nat Commun, 2023, 14(1):5552
Clin Transl Med, 2023, 13(9):e1369
Clin Transl Med, 2023, 13(9):e1369
S2290 DHA (Dihydroartemisinin) DHA (Dihydroartemisinin) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
STAR Protoc, 2024, 5(1):102896
J Exp Clin Cancer Res, 2023, 42(1):251
Antioxidants (Basel), 2023, 12(7)1468
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
MedComm (2020), 2023, 4(3):e269
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
S3022 Cabazitaxel Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
Sci Adv, 2024, 10(5):eadg7887
Cancer Drug Resist, 2024, 7:3
Biochem Pharmacol, 2023, 214:115681
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Cell Death Dis, 2024, 15(1):70
Oncogene, 2024, 43(4):235-247
Neurobiol Stress, 2024, 28:100593
S3017 Aspirin Aspirin (NSC 27223, Acetylsalicylic acid, ASA) is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.
Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
iScience, 2023, 26(7):107105
Comput Struct Biotechnol J, 2022, 20:5750-5760
S5971 Pemetrexed Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Mol Cancer Res, 2024, 22(1):82-93
Amino Acids, 2024, 56(1):15
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Sci Rep, 2023, 13(1):14453
Sci Rep, 2023, 13(1):14453
J Pers Med, 2022, 12(2)258
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
FEBS Open Bio, 2023, none
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Sci Rep, 2024, 14(1):879
Adv Sci (Weinh), 2023, 10(23):e2300898
J Thorac Oncol, 2023, S1556-0864(23)00802-X
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.
Ecotoxicol Environ Saf, 2023, 252:114608
STAR Protoc, 2023, 4(1):102122
Adv Sci (Weinh), 2022, 9(30):e2203388
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Redox Biol, 2023, 66:102845
Redox Biol, 2023, 66:102845
J Pharm Anal, 2023, 13(2):156-169
S5715 Atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.
Mol Cancer, 2023, 22(1):147
Mol Cancer, 2023, 22(1):147
Oncogene, 2023, 42(21):1716-1727
S1759 Pitavastatin calcium Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
bioRxiv, 2024, 2024.02.02.578510
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Front Oncol, 2023, 13:1287444
Cancer Res, 2022, 82(4):721-733
Clin Transl Med, 2022, 12(2):e747
S7134 IU1 IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
Cell Death Dis, 2021, 12(9):803
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
Nucleic Acids Res, 2023, gkad342
S1972 Tamoxifen Citrate Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
NAR Cancer, 2023, 5(2):zcad023
S1312 STZ (Streptozotocin) STZ (Streptozotocin) is a glucosamine-nitrosourea compound derived from Streptomyces achromogenes, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Solutions are unstable and should be fresh-prepared.
J Endocr Soc, 2024, 8(2):bvad176
Front Bioeng Biotechnol, 2023, 11:1052607
Nat Med, 2022, 10.1038/s41591-021-01645-7
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
Cell Death Discov, 2023, 9(1):97
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
JHEP Rep, 2022, 4-11:100573
S2812 (R)-(-)-Gossypol (AT-101) acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Int J Mol Sci, 2023, 24(7)6662
Cancer Cell, 2022, S1535-6108(22)00312-9
Front Oncol, 2022, 12:821620
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1576 Sulfasalazine Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
Oncogene, 2022, 41(31):3859-3875
S2751 Milciclib Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Nat Commun, 2022, 13(1):2725
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
EMBO J, 2022, 41(19):e110398
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
Life Sci Alliance, 2023, 6(8)e202302133
Cell Rep Methods, 2023, 3(10):100599
Front Pharmacol, 2022, 13:934746
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
Front Pharmacol, 2022, 13:914153
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
EMBO Rep, 2022, e53373
Cell Res, 2021, 10.1038/s41422-021-00565-y
Autophagy, 2021, 1-14
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.
J Clin Invest, 2023, 133(8)e164596
Cell Death Discov, 2023, 9(1):457
Adv Sci (Weinh), 2022, 9(27):e2105938
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Cell Mol Biol Lett, 2023, 28(1):15
PLoS Pathog, 2023, 19(3):e1011295
S1403 Tigecycline Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
EBioMedicine, 2022, 87:104397
Microorganisms, 2022, 10(7)1421
iScience, 2021, 24(11):103350
S1627 Nitazoxanide Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Biomed Pharmacother, 2024, 171:116195
Viruses, 2024, 16(2)282
iScience, 2022, 25(11):105342
S1979 Amiodarone (NSC 85442) HCl Amiodarone (NSC 85442,Amiodar,Amiodarone hydrochloride,Nexterone) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
Cell Rep Methods, 2023, 3(4):100440
Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440
Cell Mol Immunol, 2022, 19(8):925-943
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
J Pharm Sci, 2022, 111(8):2180-2190
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
Cancers (Basel), 2022, 14(9)2327
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Neurobiol Dis, 2021, 152:105294
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
S4211 Montelukast Sodium Montelukast Sodium selectively antagonizes leukotriene D4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1. Montelukast improves macroautophagy but not the chaperone-mediated autophagy pathway. Solutions are unstable and should be fresh-prepared.
Biochem Biophys Res Commun, 2022, 594:31-37
Cancer Immunol Immunother, 2021, 70(1):203-213
Aging (Albany NY), 2021, 13(24):25670-25693
S8369 Lys05 Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Sci Rep, 2024, 14(1):4000
Nat Cell Biol, 2022, 24(8):1202-1210
Adv Sci (Weinh), 2022, 9(27):e2105938
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
bioRxiv, 2020, 2020/9/20.4.7.30734
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Phytomedicine, 2023, 10.1016/j.phymed.2023.155090
Nat Genet, 2021, 53(4):435-444
J Agric Food Chem, 2021, 69(40):11847-11855
S8807 PFK158 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Nat Metab, 2022, 4(10):1287-1305
Cancers (Basel), 2022, 14(9)2113
Front Oncol, 2022, 12:826655
S1389 Omeprazole Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S3569 Spermidine Spermidine is a natural polyamine that stimulates cytoprotective macroautophagy/autophagy.
Cell Metab, 2023, S1550-4131(23)00341-8
Oxid Med Cell Longev, 2022, 2022:8033353
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S4484 Trametinib DMSO solvate Trametinib DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
PLoS One, 2022, 17(12:e0274704)
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
Anticancer Res, 2021, 41(2):687-697
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
S8240 SMER28 SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.
Nat Chem Biol, 2020, 6
Cell Rep, 2020, 31(12):107800
Cell Rep, 2019, 27(12):3413-3421
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Bone Res, 2022, 10(1):27
Cell Death Dis, 2022, 13(11):1000
iScience, 2022, 25(11):105394
S1733 Methylprednisolone Methylprednisolone (NSC-19987,U 7532) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Trop J Pharm Res, 2014, 13 (1): 53-59
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
Antiviral Res, 2016, 132:38-45
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
Nat Commun, 2023, 14(1):3997
Nat Commun, 2023, 14(1):3997
Nanomaterials (Basel), 2022, 13(1)84
S3653 Spermidine trihydrochloride Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
Cell Metab, 2023, S1550-4131(23)00341-8
Int J Mol Sci, 2021, 22(19)10255
Int J Mol Sci, 2021, 22(19), 10255
S3758 Sinomenine hydrochloride Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
Biomed Res Int, 2022, 2022:4914005
Cancer Manag Res, 2021, 13:1189-1204
Bioorg Med Chem, 2020, 31:115986
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S1837 Flubendazole Flubendazole (Flumoxanal, NSC 313680) is an autophagy inducer by targeting Atg4B, used to treat internal parasite and worm infection.
Sci Rep, 2020, 10(1):13124
RSC Advances, 2018, 10.1039/C7RA12259D
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S8576 EAD1 EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.
Mol Cancer Ther, 2022, 21(1):79-88
Autophagy, 2021, 1-17
S6650 EN6 EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein.
Cell Death Dis, 2021, 12(1):119
Brain Res, 2021, 1778:147768
S8527 ROC-325 ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
Elife, 2023, 12e83205
Adv Sci (Weinh), 2022, 9(27):e2105938
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
Biochem Biophys Res Commun, 2022, 632:40-47
Sci Adv, 2022, 8(31):eabo0412
S6301 MPP+ iodide MPP+ iodide (N-Methyl-4-Phenylpyridinium Iodide), the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces autophagic cell death in SH-SY5Y cells. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
S1041 STF-62247 STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
Neuropsychiatr Dis Treat, 2015, 11:2091-9
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
Mol Pain, 2022, 18:17448069221107810
S8764 IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Cancers (Basel), 2020, 12(9):E2363
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S3698 Nortriptyline hydrochloride Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression.
Front Bioinform, 2021, 1:710591
S6797 QX77 QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression.
Front Pharmacol, 2021, 12:707259
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S4081 Sulfacetamide Sodium Sulfacetamide Sodium is an anti-biotic.
G3 (Bethesda), 2020, 4;10(5):1585-1597
S5920 CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
J Virol, 2021, JVI0155021
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
Cell Death Discov, 2023, 9(1):109
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.
Int J Mol Sci, 2021, 23(1)17
S6395 CA77.1 CA77.1 (CA) is a potent, brain-penetrant and orally active activator of chaperone-mediated autophagy (CMA) for the treament of Alzheimer's disease (AD).
Sci Adv, 2023, 9(40):eadi8343
S9150 Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
Cell Death Dis, 2022, 13(11):1000
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
S4613 Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

S4750 Sulfacetamide sodium salt hydrate Sulfacetamide is a sulfonamide antibiotic that blocks the synthesis of dihydrofolic acid by inhibiting the enzyme dihydropteroate synthase(DHPS) with IC50 of 9.5 μM. Sulfacetamide is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), which is required for bacterial synthesis of folic acid.
S9027 Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S8744 PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
S9424 Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S3890 Leonurine Leonurine, an active alkaloid extracted from Traditional Chinese Medicine Herba leonuri, exerts several biological effects, such as antidiabetic, cardiovascular, and bovine mastitis protection.
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S4546 Xylitol Xylitol (Adonitol, Ribitol, Xylite, D-Xylitol, Adonite) is a sugar alcohol derived from XYLOSE by reduction of the carbonyl group. It is as sweet as sucrose and used as a noncariogenic sweetener.
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level.
S9310 Isorhychophylline Isorhynchophylline (IsoRhy, 7-Isorhyncophylline) is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases.
E1232 Concanavalin A Concanavalin A is a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics.
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S1105 LY294002 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
Cell Rep Med, 2024, 5(2):101420
Biomed Pharmacother, 2024, 172:116259
Stem Cell Reports, 2024, 19(2):196-210
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
S2767 3-MA (3-Methyladenine) 3-MA (3-Methyladenine) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. Solutions are unstable and should be fresh-prepared.
Bioact Mater, 2024, 32:277-291
Nat Commun, 2024, 15(1):1669
Cancer Lett, 2024, 586:216695
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
Cell Death Dis, 2024, 15(1):31
Cell Mol Life Sci, 2024, 81(1):59
mBio, 2024, e0313623.
S1150 Paclitaxel パクリタキセル (Paclitaxel (NSC 125973, PTX)) は微小管を安定化することで脱重合を阻害します。ヒト血管内皮細胞における IC50 は 0.1 pM です。
Adv Sci (Weinh), 2024, 11(5):e2305035
Cell Death Differ, 2024, 10.1038/s41418-024-01267-9
Clin Transl Med, 2024, 14(2):e1567
S1413 Bafilomycin A1 (Baf-A1) バフィロマイシン A1 (Bafilomycin A1(Baf-A1)) は液胞 H+-ATPase 阻害剤で、IC50 は 0.44 nM です。 バフィロマイシン A1 は、オートファジー (autophagy) を阻害する一方で、アポトーシス (apoptosis) を誘導することがわかっています。
Nature, 2024, 626(8000):874-880
Nat Commun, 2024, 15(1):631
Nat Commun, 2024, 15(1):1669
S1092 KU-55933 KU-55933 is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Nature, 2023, 621(7978):415-422
Circulation, 2023, 148(19):1459-1478
Nat Commun, 2023, 14(1):6088
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Antioxidants (Basel), 2024, 13(1)114
Heliyon, 2024, 10(1):e23426
J Cancer, 2024, 15(3):685-698
S1490 Ponatinib Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Clin Cancer Res, 2023, 29(16):3151-3161
Cell Death Dis, 2023, 14(7):463
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S1786 Verteporfin ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。 また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。 ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。
Bone Res, 2024, 12(1):12
Cancer Lett, 2024, 587:216692
iScience, 2024, 27(3):109125
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bioact Mater, 2024, 32:277-291
Cancer Lett, 2024, 586:216695
Basic Res Cardiol, 2024, 119(1):113-131
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Int J Mol Sci, 2024, 25(2)959
Mol Cancer, 2023, 22(1):66
Cells, 2023, 12(12)1624
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Cancer Res, 2023, 83(19):3237-3251
Biomed Pharmacother, 2023, 158:114176
Cancer Metab, 2023, 11(1):26
S2775 Nocodazole Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Life Sci Alliance, 2024, 7(4)e202302257
Nat Metab, 2023, 5(2):277-293
Adv Sci (Weinh), 2023, 10(7):e2205566
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
PLoS Pathog, 2024, 20(1):e1011958
Kidney Int, 2023, 104(5):943-955
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Iran J Basic Med Sci, 2024, 27(3):360-365.
J Radiat Res, 2024, rrad107
Research Square, 2024, 10.21203/rs.3.rs-3872267/v1
S7046 Brefeldin A (BFA) Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
Nat Commun, 2024, 15(1):203
Commun Biol, 2024, 7(1):161
Cancer Immunol Immunother, 2024, 73(1):7
S3042 Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Nat Commun, 2024, 15(1):987
Neural Regen Res, 2024, 19(1):205-211
Regen Ther, 2024, 25:229-237
S7423 KN-93 Phosphate KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration.
PLoS Pathog, 2023, 19(3):e1011295
Ren Fail, 2023, 45(1):2172961
Nat Commun, 2022, 13-1:6117
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Redox Biol, 2024, 70:103072
J Exp Clin Cancer Res, 2023, 42(1):236
J Exp Clin Cancer Res, 2023, 42(1):236
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
Biomedicines, 2023, 10.3390/biomedicines11030759
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Nat Commun, 2023, 14(1):2132
Redox Biol, 2023, 65:102833
Cell Rep, 2023, 42(2):112023
S7751 VER155008 VER155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Signal Transduct Target Ther, 2023, 8(1):229
Mol Cell, 2023, 83(15):2810-2828.e6
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Neural Regen Res, 2024, 19(1):205-211
iScience, 2024, 27(3):109166
Commun Biol, 2023, 6(1):824
S7888 Spautin-1 Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.
J Adv Res, 2024, S2090-1232(24)00025-0
Mol Cancer, 2023, 22(1):204
Nat Commun, 2023, 14(1):2691
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Cell Death Differ, 2024, 10.1038/s41418-024-01260-2
Cell Rep, 2024, 43(1):113575
PLoS Pathog, 2024, 20(1):e1011958
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Life Sci Alliance, 2023, 6(5)e202201605
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Commun, 2022, 13(1):6589
S8222 AS1842856 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
Cell Death Dis, 2023, 14(1):47
Cell Rep, 2023, 42(3):112186
Antioxidants -Basel), 2023, 12(10)1881
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Nat Commun, 2024, 15(1):1277
Sci Rep, 2024, 14(1):4000
Drug Resist Updat, 2023, 70:100985
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
S7289 PFK15 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
Nat Commun, 2023, 14(1):5552
Clin Transl Med, 2023, 13(9):e1369
Clin Transl Med, 2023, 13(9):e1369
S1835 Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
Sci Rep, 2023, 13(1):14453
Sci Rep, 2023, 13(1):14453
J Pers Med, 2022, 12(2)258
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
iScience, 2023, 26(7):107090
Heliyon, 2023, 9(3):e14169
FEBS Open Bio, 2023, none
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.
Ecotoxicol Environ Saf, 2023, 252:114608
STAR Protoc, 2023, 4(1):102122
Adv Sci (Weinh), 2022, 9(30):e2203388
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
Nucleic Acids Res, 2023, gkad342
S7660 Obeticholic Acid (INT-747) Obeticholic Acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
Phytomedicine, 2023, 119:155005
Nat Commun, 2022, 13(1):3419
JHEP Rep, 2022, 4-11:100573
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
EMBO Rep, 2022, e53373
Cell Res, 2021, 10.1038/s41422-021-00565-y
Autophagy, 2021, 1-14
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.
J Clin Invest, 2023, 133(8)e164596
Cell Death Discov, 2023, 9(1):457
Adv Sci (Weinh), 2022, 9(27):e2105938
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Immunity, 2024, 57(2):287-302.e12
Cell Rep, 2024, 43(1):113575
Sci Rep, 2024, 14(1):4000
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
S8369 Lys05 Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Sci Rep, 2024, 14(1):4000
Nat Cell Biol, 2022, 24(8):1202-1210
Adv Sci (Weinh), 2022, 9(27):e2105938
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Phytomedicine, 2023, 10.1016/j.phymed.2023.155090
Nat Genet, 2021, 53(4):435-444
J Agric Food Chem, 2021, 69(40):11847-11855
S8807 PFK158 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Nat Metab, 2022, 4(10):1287-1305
Cancers (Basel), 2022, 14(9)2113
Front Oncol, 2022, 12:826655
S1733 Methylprednisolone Methylprednisolone (NSC-19987,U 7532) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Trop J Pharm Res, 2014, 13 (1): 53-59
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
Nat Commun, 2023, 14(1):3997
Nat Commun, 2023, 14(1):3997
Nanomaterials (Basel), 2022, 13(1)84
S3758 Sinomenine hydrochloride Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
Biomed Res Int, 2022, 2022:4914005
Cancer Manag Res, 2021, 13:1189-1204
Bioorg Med Chem, 2020, 31:115986
S8576 EAD1 EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.
Mol Cancer Ther, 2022, 21(1):79-88
Autophagy, 2021, 1-17
S8527 ROC-325 ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
Elife, 2023, 12e83205
Adv Sci (Weinh), 2022, 9(27):e2105938
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
Biochem Biophys Res Commun, 2022, 632:40-47
Sci Adv, 2022, 8(31):eabo0412
S8764 IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Cancers (Basel), 2020, 12(9):E2363
S3698 Nortriptyline hydrochloride Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression.
Front Bioinform, 2021, 1:710591
S5920 CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
J Virol, 2021, JVI0155021
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.
Int J Mol Sci, 2021, 23(1)17
S9150 Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
Cell Death Dis, 2022, 13(11):1000
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
S5973 Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
S8744 PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S9424 Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
E1232 Concanavalin A Concanavalin A is a potential anti-neoplastic agent targeting apoptosis, autophagy and anti-angiogenesis for cancer therapeutics.
S1078 MK-2206 2HCl MK-2206 2HCl は高い選択性をもつ Akt1/2/3 阻害剤であり、cell-free assay における IC50 はそれぞれ 8 nM/ 12 nM/ 65 nM です。一方で、他の250種におよぶキナーゼ (kinases) に対しては活性が検出されていません。MK-2206 2HCl はがん細胞におけるオートファジー (autophagy) アポトーシス (apoptosis) に関与します。臨床第2相試験中
Nat Commun, 2024, 15(1):686
Cell Rep Med, 2024, 5(2):101420
Int J Biol Sci, 2024, 20(4):1389-1409
S1039 Rapamycin (Sirolimus) ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。
Drug Resist Updat, 2024, 73:101063
Cell Rep Med, 2024, 5(2):101420
J Adv Res, 2024, S2090-1232(24)00079-1
S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
Cell, 2024, 187(4):945-961.e18
Nat Commun, 2024, 15(1):866
Cell Rep Med, 2024, 5(2):101396
S1049 Y-27632 2HCl Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):827
S1263 Laduviglusib (CHIR-99021) ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S1120 Everolimus エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。
Cell, 2024, 187(3):712-732.e38
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
S1025 Gefitinib Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Gastroenterology, 2024, S0016-5085(24)00062-3
Phytomedicine, 2024, 125:155351
mBio, 2024, e0228723.
S1166 Cisplatin シスプラチン (Cisplatin (NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP)) は無機白金錯体であり、腫瘍細胞中において DNA 付加物を形成することにより DNA 合成を阻害する能力を有します。シスプラチンはフェロトーシス (ferroptosis) を活性化し、オートファジー (autophagy) を誘導します。溶液は都度調製してください。DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.Solutions are unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):866
Clin Cancer Res, 2024, 30(1):187-197
Cancer Lett, 2024, 586:216695
S1267 Vemurafenib (PLX4032) Vemurafenib (RG7204, RO5185426,PLX4032) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
Biochem Pharmacol, 2024, 219:115952
Nat Cancer, 2023, 4(2):240-256
Nat Commun, 2023, 14(1):3251
S1378 Ruxolitinib ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
Acta Neuropathol, 2024, 147(1):28
Theranostics, 2024, 14(3):1224-1240
Cell Rep, 2024, 43(2):113600.
S1023 Erlotinib HCl Erlotinib HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Nat Commun, 2023, 14(1):1559
Nat Commun, 2023, 14(1):7863
Cell Rep, 2023, 42(8):112868
S7786 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
NPJ Precis Oncol, 2024, 8(1):3
Transl Oncol, 2024, 39:101834
J Biol Chem, 2024, S0021-9258(24)00139-X
S8048 Venetoclax (ABT-199) Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.
Nat Commun, 2024, 15(1):1821
Cell Death Dis, 2024, 15(2):131
Cell Death Discov, 2024, 10(1):35
S1047 Vorinostat (SAHA) Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.
Cell Rep, 2024, 43(1):113575
NPJ Precis Oncol, 2024, 8(1):52
Clin Epigenetics, 2024, 16(1):13
S1021 Dasatinib Dasatinibは新規の強力なマルチターゲット阻害剤であり、cell-free assy における Abl, Src および c-Kit に対する IC50 はそれぞれ < 1 nM, 0.8 nM および 79 nM です。Dsatinib はオートファジー (autophagy)アポトーシス (apoptosis) を誘発し、抗腫瘍活性を示します。
Nature, 2024, 10.1038/s41586-024-07079-8
Cell Rep Med, 2024, 5(2):101416
Cell Rep Med, 2024, 5(2):101412
S1250 Enzalutamide エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。
Cancers (Basel), 2024, 16(2)296
bioRxiv, 2024, 10.1101/2024.01.16.575611
bioRxiv, 2024, 10.1101/2023.12.01.569685
S7397 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Genomics, 2024, 116(1):110764
Mol Cell, 2023, 83(5):803-818.e8
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Adv Sci (Weinh), 2024, 11(4):e2304987
Genome Biol, 2024, 25(1):58
Cell Death Discov, 2024, 10(1):95
S2111 Lapatinib Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Drug Resist Updat, 2024, 73:101066
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 10.1038/s41467-023-39059-3
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):5242
J Clin Invest, 2023, 133(18)e168352
S1068 Crizotinib Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S7840 Dorsomorphin Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
iScience, 2024, 27(2):108852
J Ethnopharmacol, 2024, 324:117814
J Cell Mol Med, 2024, 28(2):e18055
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
NPJ Precis Oncol, 2024, 8(1):52
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Cancer Res Commun, 2024, 4(2):349-364
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Cell Rep, 2024, 43(1):113575
Int J Mol Sci, 2024, 25(2)1278
Cancer Res Commun, 2024, 4(2):349-364
S1011 Afatinib アファチニブ (Afatinib) は in vitro において EGFR/ErbB を不可逆的に阻害します。IC50 は EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4) に対してそれぞれ 0.5, 0.4, 10, 14 および 1 nM です。アファチニブによってオートファジー (autophagy) が誘発されることが報告されています。
Cell, 2024, 187(3):712-732.e38
Cell Rep, 2024, 43(1):113614
NPJ Precis Oncol, 2024, 8(1):3
S7110 (+)-JQ1 (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Gastroenterology, 2024, S0016-5085(24)00062-3
bioRxiv, 2024, 2024.01.29.577409
Cell Discov, 2023, 9(1):47
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Sci Rep, 2024, 14(1):4303
bioRxiv, 2024, 2024.01.17.575938
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):830
Nat Commun, 2024, 15(1):1041
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Nat Commun, 2024, 15(1):1300
Nat Cancer, 2023, 4(2):240-256
Cancer Res, 2023, 83(1):141-157
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575847
Cancer Discov, 2023, 13(7):1696-1719
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S2475 Imatinib Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy.
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
Cell Commun Signal, 2023, 21(1):342
Phytomedicine, 2023, 117:154918
S2226 Idelalisib (CAL-101) Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Transl Oncol, 2024, 43:101857
Cancer Cell, 2023, 41(6):1103-1117.e12
Nat Cancer, 2023, 4(10):1508-1525
S1040 Sorafenib tosylate Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Cell, 2023, S0092-8674(23)01032-2
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
J Biol Chem, 2024, S0021-9258(24)00057-7
Nat Neurosci, 2023, none
S1714 Gemcitabine Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2024, 15(1):1287
Genes Dis, 2024, 11(1):430-448
iScience, 2024, 27(1):108667
S1026 Imatinib Mesylate Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.04.574149
Cell Rep Med, 2023, 4(5):101025
Blood Cancer J, 2023, 13(1):42
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Cell Death Discov, 2024, 10(1):74
EMBO Mol Med, 2023, e16235.
Cell Syst, 2023, S2405-4712(23)00116-3
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Pharmaceuticals (Basel), 2024, 17(1)77
Heliyon, 2024, 10(3):e24779
Mol Neurodegener, 2023, 18(1):67
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Int J Chron Obstruct Pulmon Dis, 2024, 19:269-279
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
J Transl Med, 2024, 22(1):208
iScience, 2024, 27(2):109015.
Cell Discov, 2023, 9(1):47
S1224 Oxaliplatin Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Mol Cancer, 2024, 23(1):23
Gastroenterology, 2024, S0016-5085(24)00062-3
NPJ Precis Oncol, 2024, 8(1):52
S1178 Regorafenib Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。
Nat Med, 2024, 10.1038/s41591-024-02824-y
NPJ Precis Oncol, 2024, 8(1):52
Signal Transduct Target Ther, 2023, 8(1):65
S1237 TMZ(Temozolomide) テモゾロミド (Temozolomide (NSC 362856,TMZ,CCRG 81045,Methazolastone)) はDNA 環上の窒素原子と環外酸素を修飾することが可能な単官能性 SN1 アルキル化剤であり、中間体である MTIC を経て、活性代謝産物であるメチルジアゾニウムカチオン (methyl diazoniumcation) に分解されると、生理学的 pH において DNA にメチル基を転移します。テモゾロミドはアポトーシス (apoptosis) を誘発し、抗がん活性を呈します。L-1210 細胞および L-1210/BCNU 細胞における DNA 損傷誘導剤です。
Cancer Cell Int, 2024, 24(1):36
bioRxiv, 2024, 2024.01.20.576487.
Research Square, 2024, 10.21203/rs.3.rs-3886648/v1
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Virol J, 2024, 21(1):23
Int J Mol Sci, 2023, 24(7)6228
Front Oncol, 2023, 13:1043694
S1130 Sepantronium Bromide (YM155) Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Adv Sci (Weinh), 2023, 10(25):e2301753
Cell Rep Med, 2023, 4(12):101339
Proc Natl Acad Sci U S A, 2023, 120(4):e2218118120
S1129 SRT1720 HCl SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3. SRT1720 induces autophagy.
bioRxiv, 2024, 10.1101/2024.01.21.576539
Chinese Journal of Tissue Engineering Research, 2024, (28): 4447-4454.
Small, 2023, e2300584.
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Cell Rep Med, 2024, 5(2):101396
Theranostics, 2024, 14(4):1561-1582
Clin Transl Med, 2024, 14(2):e1583
S1149 Gemcitabine HCl ゲムシタビン塩酸塩 (Gemcitabine (LY-188011, NSC 613327) HCl) は DNA 合成阻害剤であり、 PANC1 細胞、 MIAPaCa2 細胞、 BxPC3 細胞および Capan2 細胞における IC50 はそれぞれ 50 nM, 40 nM, 18nM, 12 nM です。
Int J Biol Sci, 2024, 20(4):1389-1409
Phytomedicine, 2024, 155377
Neoplasia, 2024, 47:100951
S7810 Afatinib Dimaleate Afatinib Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
J Invest Dermatol, 2024, S0022-202X(23)03210-4
RSC Adv, 2023, 13(16):11037-11043
Biochem Biophys Rep, 2023, 34:101436
S1582 H 89 2HCl H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM in a cell-free assay, 10-fold selective for PKA than PKG,500-fold greater selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. H 89 2HCl induces autophagy.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Commun Signal, 2024, 22(1):48
iScience, 2024, 27(3):109125
S1191 Fulvestrant フルベストラント (Fulvestrant (ICI-182780, ZD 9238, ZM 182780)) はエストロゲン受容体 (estrogen receptor, ER) アンタゴニストであり、cell-free assay における IC50 は 0.94 nM です。フルベストラントはまたオートファジー (autophagy)アポトーシス (apoptosis) を誘導し、抗腫瘍活性を呈します。
Cancers (Basel), 2024, 16(3)678
Cancers (Basel), 2024, 16(2)257
bioRxiv, 2024, 10.1101/2024.01.16.575899
S2449 Forskolin (Colforsin) コルホルチン (Forskolin (Colforsin)) は、広範な細胞腫における真核生物のアデニル酸シクラーゼ (adenylate cyclase, AC) の遍在する活性化因子であり、細胞生理学の研究において cAMP のレベルを上げるために一般的に使用されています。ホルスコリン (Forskolin) は、PXRFXR も活性化します。 ホルスコリンはオートファジー (autophagy) を刺激します。
iScience, 2024, 27(2):108857
bioRxiv, 2024, 2024.01.15.574730
Cell Stem Cell, 2023, 30(7):938-949.e7
S1033 Nilotinib Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Nat Commun, 2024, 15(1):651
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
NPJ Precis Oncol, 2023, 7(1):132
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Signal Transduct Target Ther, 2023, 8(1):183
Nucleic Acids Res, 2023, 51(9):4451-4466
Autophagy, 2023, 10.1080/15548627.2023.2281128
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
Cell Death Dis, 2024, 15(1):35
Sci Adv, 2024, 10(8):eadk3663
Signal Transduct Target Ther, 2023, 8(1):229
S1014 Bosutinib Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Heliyon, 2024, 10(1):e23690
Mol Cell, 2023, 83(5):803-818.e8
Cancer Res, 2023, 83(1):141-157
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Neoplasia, 2024, 48:100966
Nat Commun, 2023, 14(1):6505
S1230 Flavopiridol (Alvocidib) Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Nat Commun, 2024, 15(1):35
Elife, 2024, 13e80684
Nat Genet, 2023, 55(10):1721-1734
S2929 Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
Cell Death Dis, 2023, 14(10):672
iScience, 2023, 26(7):107090
Int J Mol Sci, 2023, 24(20)15258
S1057 Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.
bioRxiv, 2024, 10.1101/2023.01.18.524628
Emerg Microbes Infect, 2022, 1-29
Cancers (Basel), 2022, 14(22)5602
S1046 Vandetanib Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Nat Cancer, 2023, 4(9):1345-1361
Cell Reports, 2023, 112328
Cell Rep, 2023, 42(4):112328
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
J Invest Dermatol, 2024, S0022-202X(23)03210-4
Clin Epigenetics, 2024, 16(1):13
Nat Commun, 2023, 14(1):5051
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Sci Adv, 2024, 10(8):eadk3663
bioRxiv, 2024, 10.1101/2024.01.16.575190
Adv Sci (Weinh), 2023, 10.1002/advs.202302025
S1782 Azacitidine (5-Azacytidine) Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Nat Commun, 2024, 15(1):1750
Cell Rep Med, 2024, 5(2):101416
Biochem Pharmacol, 2024, S0006-2952(24)00048-0
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Nat Commun, 2023, 14(1):390
Aging Cell, 2023, e13888.
BMC Cancer, 2023, 23(1):499
S1085 Belinostat Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Cell Rep, 2024, 43(1):113575
Clin Epigenetics, 2023, 15(1):19
Transl Oncol, 2023, 39:101779
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Comput Struct Biotechnol J, 2023, 21:1157-1168
Mol Cell Biol, 2023, 43(1):1-21
J Cell Commun Signal, 2023, 17(3):975-989
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Cell Commun Signal, 2024, 22(1):117
Mol Carcinog, 2024, 63(3):430-447
Research Square, 2024, 10.21203/rs.3.rs-3834927/v1
S1322 Dexamethasone Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Cell Host Microbe, 2024, S1931-3128(24)00005-2
Oncogene, 2024, 43(4):235-247
bioRxiv, 2024, 2024.01.29.577409
S8075 GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Acta Pharm Sin B, 2023, 13(6):2601-2612
Cell Death Dis, 2023, 14(7):461
Cell Death Dis, 2023, 14(12):830
S1075 SB216763 SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
Cell Death Dis, 2023, 14(8):500
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
PLoS One, 2024, 19(1):e0295629
Cancer Res Commun, 2024, 4(2):349-364
J Cell Biol, 2023, 222(2)e202205092
S5003 Tacrolimus (FK506) Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Nat Commun, 2023, 14(1):3928
Cell Commun Signal, 2023, 21(1):25
JCI Insight, 2023, 8(14)e157027
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Clin Respir J, 2024, 18(1):e13731
Cell Death Dis, 2023, 14(7):469
Cell Death Dis, 2023, 14(7):469
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Gastroenterology, 2024, S0016-5085(24)00062-3
Oncologist, 2024, 29(1):15-24
Cell Rep Med, 2023, 4(4):101002
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
S7655 Telaglenastat (CB-839) CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1.
Signal Transduct Target Ther, 2023, 8(1):159
Cancer Discov, 2023, 13(7):1696-1719
J Thorac Oncol, 2023, S1556-0864(23)00197-1
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
bioRxiv, 2024, 2024.02.06.579216
Nat Commun, 2023, 14(1):6088
Nat Commun, 2023, 14(1):4991
S1648 Cytarabine Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Int J Mol Sci, 2024, 25(1)646
Cell Signal, 2024, 114:111004
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines.
Cell Death Dis, 2023, 14(4):234
JCI Insight, 2023, 8(23)e164968
Phytomedicine, 2023, 115:154809
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
PLoS One, 2024, 19(1):e0295629
bioRxiv, 2024, 2024.01.20.576487.
Mol Cell, 2023, 83(13):2206-2221.e11
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
S5742 Deferoxamine mesylate Deferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.Please do not prepare stock solutions with normal saline or PBS, as precipitation may occur.
Redox Biol, 2024, 69:103008
Ecotoxicol Environ Saf, 2024, 270:115889
J Cancer, 2024, 15(3):685-698
S1017 Cediranib (AZD2171) Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Cell Oncol (Dordr), 2023, 46(2):391-407
Biochem Pharmacol, 2023, 214:115681
Int J Mol Sci, 2023, 24(9)8037
S2180 Ixazomib (MLN2238) Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
iScience, 2023, 26(8):107302
iScience, 2023, 26(8):107302
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
NPJ Precis Oncol, 2024, 8(1):52
Cancer Discov, 2023, 13(10):2192-2211
Cancer Discov, 2023, 13(10):2192-2211
S8964 Actinomycin D (Dactinomycin) Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
Cell Mol Life Sci, 2024, 81(1):92
NPJ Precis Oncol, 2024, 8(1):22
Signal Transduct Target Ther, 2023, 8(1):63
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Theranostics, 2024, 14(4):1561-1582
Acta Biomater, 2024, S1742-7061(24)00036-9
Int J Biol Sci, 2024, 20(2):784-800
S1396 Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
S2285 Cryptotanshinone (Tanshinone C) Cryptotanshinone (Tanshinone C) is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
J Med Virol, 2023, 95(11):e29230
Microbiol Spectr, 2023, e0493222.
Evid Based Complement Alternat Med, 2023, 2023:1307323
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
S1792 Simvastatin Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
Neuron, 2023, S0896-6273(23)00513-5
Cancer Res, 2023, 83(13):2248-2261
Cell Death Dis, 2023, 14(4):234
S2556 Rosiglitazone Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Nat Commun, 2024, 15(1):1429
J Hematol Oncol, 2023, 16(1):30
EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cancer Cell Int, 2024, 24(1):43
J Transl Med, 2023, 21(1):530
J Transl Med, 2023, 21(1):530
S2799 Daporinad (FK866) Daporinad (FK866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.
Nat Commun, 2023, 14(1):6246
Nat Commun, 2023, 14(1):6246
Endocrinology, 2023, 164(6)bqad073
S1035 Pazopanib HCl Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.
iScience, 2023, 26(7):107116
NPJ Breast Cancer, 2022, 8(1):44
J Pers Med, 2022, 12(2)258
S2679 Flavopiridol (Alvocidib) HCl Flavopiridol (Alvocidib) HClcompetes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
Elife, 2024, 13e80684
Int J Biol Macromol, 2023, 258(Pt 1):128776
Mol Cell Biol, 2023, 43(1):1-21
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
J Exp Clin Cancer Res, 2023, 42(1):8
Cell Death Dis, 2023, 14(10):652
Cell Death Dis, 2023, 14(10):652
S1238 Tamoxifen Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Nat Commun, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
S1314 Zoledronic acid (Zoledronate) Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Nat Commun, 2023, 14(1):1413
Nature Communications, 2023, 1413-2023)
Cancers (Basel), 2023, 15(3)610
S2843 BI-D1870 BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
BMC Cancer, 2024, 24(1):233
Leukemia, 2023, 37(8):1611-1625
Leukemia, 2023, 37(8):1611-1625
S2163 PF-4708671 PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.
Adv Sci (Weinh), 2023, 10(3):e2203718
Nucleic Acids Res, 2023, 51(22):12076-12091
CNS Neurosci Ther, 2023, 10.1111/cns.14475
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
J Immunother Cancer, 2023, 11(11)e007736
Clin Transl Med, 2023, 13(12):e1502
J Neuroinflammation, 2023, 20(1):168
S7130 PR-619 PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.
Nat Commun, 2024, 15(1):1642
J Nanobiotechnology, 2023, 21(1):117
Ecotoxicol Environ Saf, 2023, 263:115197
S8047 Dynasore Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).
Immunity, 2024, 57(2):287-302.e12
Nat Commun, 2024, 15(1):1669
J Exp Med, 2023, 220(3)e20221316
S7842 LY3009120 LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.
Drug Resist Updat, 2023, 71:100993
Exp Cell Res, 2023, 430(1):113722
Sci Adv, 2023, 9(28):eadf4766
S1190 Bicalutamide Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Cancers (Basel), 2024, 16(2)296
Biomedicines, 2024, 12(1)181
J Exp Clin Cancer Res, 2023, 42(1):204
S2061 Lovastatin Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent). Lovastatin triggers autophagy.
DNA Repair (Amst), 2024, 134:103627
bioRxiv, 2024, 10.1101/2024.01.16.575899
Signal Transduct Target Ther, 2023, 8(1):183
S1590 TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.
Sci Rep, 2024, 14(1):5038
Stem Cells Transl Med, 2023, szad085
J Nanobiotechnology, 2022, 20(1):148
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.
Mol Cell, 2023, 83(13):2206-2221.e11
J Transl Med, 2023, 21(1):115
Biochem Pharmacol, 2023, 214:115681
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Cell Rep, 2023, 42(8):112925
bioRxiv, 2023, 2023.01.17.524444
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cell Rep, 2023, 42(9):113067
Breast Cancer Res, 2023, 25(1):51
Adv Skin Wound Care, 2023, 36(5):249-258
S7998 Entrectinib Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Biomolecules, 2023, 13(3)438
S3030 Niclosamide Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
Int J Nanomedicine, 2023, 18:7505-7521
Front Cell Dev Biol, 2023, 11:1062229
J Am Heart Assoc, 2023, 12(1):e027222
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.
Mol Cancer, 2023, 22(1):64
Int J Mol Sci, 2023, 24(6)5464
Molecules, 2022, 27(19)6149
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Dev Cell, 2023, 58(6):506-521.e5
Cell Death Dis, 2023, 14(9):627
Cell Death Dis, 2023, 14(9):627
S1135 Pemetrexed disodium Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Cancer Cell, 2022, 40(10):1128-1144.e8
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
S7483 DMOG DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.
Nucleic Acids Res, 2023, gkad796
Redox Biol, 2023, 66:102858
EMBO J, 2023, 42(20):e113743
S1896 Hydroxyurea Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
bioRxiv, 2024, 10.1101/2024.01.04.574133
Cell Rep, 2023, 42(7):112660
Cell Rep, 2023, 42(10):113176
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
S2391 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
MedComm (2020), 2023, 4(5):e346
MedComm -2020), 2023, 4(5):e346
Aging Cell, 2023, e13771.
S4505 Vinblastine sulfate Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
J Immunother Cancer, 2023, 11(8)e007253
J Immunother Cancer, 2023, 10.1136/jitc-2023-007253
Cell Rep, 2023, 42(4):112324
S4269 Vinorelbine ditartrate Vinorelbine ditartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cell Rep, 2023, 42(10):113176
J Pathol, 2023, 261(3):256-268
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00786-w
S1235 Letrozole Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays.It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. Letrozole induces autophagy.
Mol Oncol, 2023, 10.1002/1878-0261.13541
Commun Biol, 2023, 6(1):695
Nature Communications, 2022, 13, 5258
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1.
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
Sci Rep, 2022, 12(1):6345
S7104 AZD1208 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Angiogenesis, 2024, 10.1007/s10456-024-09906-y
Mol Cancer, 2023, 22(1):64
Cell Rep, 2023, S2211-1247(23)00893-8
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Cell Rep, 2022, 38(9):110448
Front Pharmacol, 2022, 13:1032975
J Pers Med, 2022, 12(2)258
S2713 Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
Int J Mol Sci, 2023, 24(18)13830
ACS Cent Sci, 2022, 8(5):636-655
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cell Death Discov, 2023, 9(1):57
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
S1168 Valproic Acid sodium Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Sci Total Environ, 2022, 838(Pt 2):155825
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
Transl Psychiatry, 2022, 12(1):130
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
Nat Commun, 2022, 13(1):2500
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
Nat Commun, 2023, 14(1):886
Environ Pollut, 2023, 323:121306
Exp Gerontol, 2023, 173:112091
S3944 VPA (Valproic acid) VPA (Valproic acid) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Nat Commun, 2024, 15(1):668
Cell Mol Life Sci, 2024, 81(1):92
Cell Death Discov, 2024, 10(1):95
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Int J Nanomedicine, 2023, 18:4313-4327
Exp Gerontol, 2023, 173:112091
Cell Death Differ, 2022, 10.1038/s41418-022-01053-5
S4028 Dexamethasone Sodium Phosphate Dexamethasone (Dexamethasone 21-phosphate disodium salt) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Pharmaceutics, 2022, 14(2)400
Front Oncol, 2022, 12:888695
Sci Rep, 2022, 12(1):10616
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
S2782 GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
Mol Metab, 2024, 79:101841
Chin Med, 2024, 19(1):16
Nat Commun, 2023, 14(1):2656
S2505 Rosiglitazone maleate Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Stem Cell Reports, 2022, 17(11):2531-2547
Cell Death Dis, 2021, 12(11):972
Antioxidants (Basel), 2021, 10(2)155
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
J Clin Invest, 2023, 133(18)e166490
J Clin Invest, 2023, 133(18)e166490
Aging Cell, 2023, 22(6):e13840
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Acta Pharm Sin B, 2023, 13(6):2601-2612
J Exp Clin Cancer Res, 2023, 42(1):320
Pharmacol Res, 2022, 177:106122
S7177 PF-543 hydrochloride PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy.
J Transl Med, 2024, 22(1):43
Int J Mol Sci, 2023, 24(9)8303
Cell Res, 2022, 10.1038/s41422-022-00614-0
S2290 DHA (Dihydroartemisinin) DHA (Dihydroartemisinin) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
STAR Protoc, 2024, 5(1):102896
J Exp Clin Cancer Res, 2023, 42(1):251
Antioxidants (Basel), 2023, 12(7)1468
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
MedComm (2020), 2023, 4(3):e269
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
S3022 Cabazitaxel Cabazitaxel is a semi-synthetic derivative of a natural taxoid that kills cancer cells by inhibiting cell division and growth. Cabazitaxel exerts its effects by inhibiting microtubule growth and assembly, processes that are essential for cells to divide. Cabazitaxel induces autophagy via the PI3K/Akt/mTOR pathway.
Sci Adv, 2024, 10(5):eadg7887
Cancer Drug Resist, 2024, 7:3
Biochem Pharmacol, 2023, 214:115681
S2606 Mifepristone Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Cell Death Dis, 2024, 15(1):70
Oncogene, 2024, 43(4):235-247
Neurobiol Stress, 2024, 28:100593
S3017 Aspirin Aspirin (NSC 27223, Acetylsalicylic acid, ASA) is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.
Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
iScience, 2023, 26(7):107105
Comput Struct Biotechnol J, 2022, 20:5750-5760
S5971 Pemetrexed Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
Mol Cancer Res, 2024, 22(1):82-93
Amino Acids, 2024, 56(1):15
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Sci Rep, 2024, 14(1):879
Adv Sci (Weinh), 2023, 10(23):e2300898
J Thorac Oncol, 2023, S1556-0864(23)00802-X
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Redox Biol, 2023, 66:102845
Redox Biol, 2023, 66:102845
J Pharm Anal, 2023, 13(2):156-169
S5715 Atorvastatin Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.
Mol Cancer, 2023, 22(1):147
Mol Cancer, 2023, 22(1):147
Oncogene, 2023, 42(21):1716-1727
S1759 Pitavastatin calcium Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
bioRxiv, 2024, 2024.02.02.578510
bioRxiv, 2024, 10.1101/2024.01.16.575899
Nat Commun, 2023, 14(1):3251
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Front Oncol, 2023, 13:1287444
Cancer Res, 2022, 82(4):721-733
Clin Transl Med, 2022, 12(2):e747
S7134 IU1 IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
Cell Death Dis, 2021, 12(9):803
S1972 Tamoxifen Citrate Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
RNA, 2023, 29(9):1325-1338.
RNA, 2023, rna.079509.122
NAR Cancer, 2023, 5(2):zcad023
S1312 STZ (Streptozotocin) STZ (Streptozotocin) is a glucosamine-nitrosourea compound derived from Streptomyces achromogenes, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Solutions are unstable and should be fresh-prepared.
J Endocr Soc, 2024, 8(2):bvad176
Front Bioeng Biotechnol, 2023, 11:1052607
Nat Med, 2022, 10.1038/s41591-021-01645-7
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
JCI Insight, 2023, 8(15)e167440
JCI Insight, 2023, 8(15)e167440
Cell Death Discov, 2023, 9(1):97
S2812 (R)-(-)-Gossypol (AT-101) acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Int J Mol Sci, 2023, 24(7)6662
Cancer Cell, 2022, S1535-6108(22)00312-9
Front Oncol, 2022, 12:821620
S3031 Linagliptin (GSK2118436) Linagliptin (GSK2118436) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1576 Sulfasalazine Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Cancers (Basel), 2023, 10.3390/cancers15225424
Cancer Res, 2022, canres.1707.2021
Oncogene, 2022, 41(31):3859-3875
S2751 Milciclib Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2.
Nat Commun, 2022, 13(1):2725
Eur J Pharm Sci, 2021, 159:105740
Eur J Pharm Sci, 2021, S0928-0987(21)00042-7
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
EMBO J, 2022, 41(19):e110398
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
Life Sci Alliance, 2023, 6(8)e202302133
Cell Rep Methods, 2023, 3(10):100599
Front Pharmacol, 2022, 13:934746
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
Front Pharmacol, 2022, 13:914153
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
Cancers (Basel), 2022, 14(2)282
S7343 URMC-099 URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy.
Cell Commun Signal, 2023, 21(1):82
Oncogene, 2023, 42(14):1132-1143.
Oncogenesis, 2023, 12(1):35
S1403 Tigecycline Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline induces autophagy by downregulating the PI3K-AKT-mTOR pathway.
EBioMedicine, 2022, 87:104397
Microorganisms, 2022, 10(7)1421
iScience, 2021, 24(11):103350
S1979 Amiodarone (NSC 85442) HCl Amiodarone (NSC 85442,Amiodar,Amiodarone hydrochloride,Nexterone) HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.
Cell Rep Methods, 2023, 3(4):100440
Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440
Cell Mol Immunol, 2022, 19(8):925-943
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
J Pharm Sci, 2022, 111(8):2180-2190
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
Cancers (Basel), 2022, 14(9)2327
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Neurobiol Dis, 2021, 152:105294
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Biol Chem, 2023, 299(4):103017
Microbiol Spectr, 2023, 11(4):e0055223
Nat Commun, 2022, 13(1):7113
S4211 Montelukast Sodium Montelukast Sodium selectively antagonizes leukotriene D4 (LTD4) by binding to it so that block the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1. Montelukast improves macroautophagy but not the chaperone-mediated autophagy pathway. Solutions are unstable and should be fresh-prepared.
Biochem Biophys Res Commun, 2022, 594:31-37
Cancer Immunol Immunother, 2021, 70(1):203-213
Aging (Albany NY), 2021, 13(24):25670-25693
S2480 Loperamide HCl Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Front Cell Infect Microbiol, 2023, 13:1139152
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
bioRxiv, 2020, 2020/9/20.4.7.30734
S1389 Omeprazole Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S3569 Spermidine Spermidine is a natural polyamine that stimulates cytoprotective macroautophagy/autophagy.
Cell Metab, 2023, S1550-4131(23)00341-8
Oxid Med Cell Longev, 2022, 2022:8033353
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S4484 Trametinib DMSO solvate Trametinib DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
JID Innov, 2024, 4(2):100248
Cell Rep, 2022, 38(7):110374
Mol Cell Proteomics, 2022, 21(6):100240
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces autophagy. Phase 3.
iScience, 2023, 26(6):106997
J Dermatol Sci, 2022, S0923-1811(22)00125-6
PLoS One, 2022, 17(12:e0274704)
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
Anticancer Res, 2021, 41(2):687-697
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Nucleic Acids Res, 2023, gkad001
Cancer Lett, 2022, 544:215812
Cell Death Dis, 2022, 13(5):450
S8240 SMER28 SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.
Nat Chem Biol, 2020, 6
Cell Rep, 2020, 31(12):107800
Cell Rep, 2019, 27(12):3413-3421
S1747 Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.
Cell Discov, 2020, 6(1):96
G3 (Bethesda), 2020, 4;10(5):1585-1597
Antiviral Res, 2016, 132:38-45
S3653 Spermidine trihydrochloride Spermidine (4-Azaoctamethylenediamine), a natural polyamine produced from putrescine and decarboxylated S-adenosylmethionine (dcSAM) by spermidine synthase, is a novel autophagy inducer and negatively modulates N-methyl-d-aspartate (NMDA).
Cell Metab, 2023, S1550-4131(23)00341-8
Int J Mol Sci, 2021, 22(19)10255
Int J Mol Sci, 2021, 22(19), 10255
S8432 Troglitazone Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S1837 Flubendazole Flubendazole (Flumoxanal, NSC 313680) is an autophagy inducer by targeting Atg4B, used to treat internal parasite and worm infection.
Sci Rep, 2020, 10(1):13124
RSC Advances, 2018, 10.1039/C7RA12259D
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Cell Mol Life Sci, 2023, 80(11):333
Drug Dev Res, 2022, 10.1002/ddr.21927
S6650 EN6 EN6 is a novel covalent autophagy activator and targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase with an IC50 of 1.7 μM for recombinant human ATP6V1A protein.
Cell Death Dis, 2021, 12(1):119
Brain Res, 2021, 1778:147768
S6847 ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.
PLoS Pathog, 2023, 19(3):e1011295
J Mol Endocrinol, 2019, 63(3):199-213
S6301 MPP+ iodide MPP+ iodide (N-Methyl-4-Phenylpyridinium Iodide), the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces autophagic cell death in SH-SY5Y cells. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
S2458 Clonidine HCl Clonidine HCl(Kapvay) is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
Mol Pain, 2022, 18:17448069221107810
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S6797 QX77 QX77 is a novel activator of chaperone-mediated autophagy (CMA). QX77 induces the up-regulation of Rab11 expression and up-regulates LAMP2A expression.
Front Pharmacol, 2021, 12:707259
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
Front Pharmacol, 2022, 13:795613
S4081 Sulfacetamide Sodium Sulfacetamide Sodium is an anti-biotic.
G3 (Bethesda), 2020, 4;10(5):1585-1597
S6078 ICCB-19 hydrochloride ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
Cell Death Discov, 2023, 9(1):109
S6395 CA77.1 CA77.1 (CA) is a potent, brain-penetrant and orally active activator of chaperone-mediated autophagy (CMA) for the treament of Alzheimer's disease (AD).
Sci Adv, 2023, 9(40):eadi8343
S2491 Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
S4613 Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S1027 FL-411 FL-411 (BRD4-IN-1) is a potent and selective inhibitor of Bromodomain-containing protein 4 (BRD4) with IC50 of 0.43 μM for BRD4(1). FL-411 induces ATG5-dependent autophagy-associated cell death (ACD) by blocking BRD4-AMPK interaction.
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

S9027 Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
S4476 PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S6851 RA-190 RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
S4546 Xylitol Xylitol (Adonitol, Ribitol, Xylite, D-Xylitol, Adonite) is a sugar alcohol derived from XYLOSE by reduction of the carbonyl group. It is as sweet as sucrose and used as a noncariogenic sweetener.
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level.
S9310 Isorhychophylline Isorhynchophylline (IsoRhy, 7-Isorhyncophylline) is a major tetracyclic oxindole alkaloid isolated from the Chinese herbal medicine Uncaria rhynchophylla (Miq.)Jacks (Gouteng in Chinese). It acts as a neuronal autophagy inducer with therapeutic potential for cardiovascular and central nervous system diseases.
S7307 GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Exp Mol Med, 2024, 56(2):408-421.
Cell Discov, 2023, 9(1):7
Cell Death Dis, 2023, 14(7):467
S8597 LYN-1604 LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
J Virol, 2021, JVI0155021
Exp Eye Res, 2019, 184:126-134
S2924 Laduviglusib (CHIR-99021) HCl ラドゥビグルシブ塩酸塩 (Laduviglusib (CHIR-99021; CT99021) HCl) は CHIR-99021 の塩酸塩で、GSK-3α/β 阻害剤 (IC50 = 10 nM/6.7 nM) です。 CHIR-99021 は、最も近縁なホモログである Cdc2 および ERK2 と比較して、GSK-3 に対して 500 倍を超える選択性を示します。 CHIR-99021 は、Wnt/β-カテニン シグナル伝達経路の強力な薬理学的活性化因子です。 CHIR-99021 は、光誘発されるオートファジー (autophagy) を大幅にレスキューし、GR、RORα、およびオートファジー関連タンパク質量を増大します。
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
S2215 DAPT DAPT (GSI-IX、LY-374973) は新規の γ-セクレターゼ 阻害剤であり、HEK 293 細胞で 20 nM の IC50 で Aβ 産生を阻害します。 DAPT はヒト舌癌細胞のアポトーシス(apoptosis) を促進し、オートファジー (autophagy) を調節します。
Genome Biol, 2024, 25(1):58
Br J Cancer, 2024, 10.1038/s41416-024-02576-z
Antibodies (Basel), 2024, 13(1)15
S1241 Vincristine sulfate Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
iScience, 2024, 27(1):108667
Cell Rep Med, 2023, 4(12):101339
Acta Neuropathol Commun, 2023, 11(1):6
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
Cell Stem Cell, 2024, S1934-5909(24)00041-9
Sci Rep, 2024, 14(1):4060
Mol Cancer, 2023, 22(1):204
S1274 BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S1204 Melatonin Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Ecotoxicol Environ Saf, 2023, 255:114719
Microbiol Res, 2023, 276:127480
Cell Oncol (Dordr), 2023, 10.1007/s13402-023-00875-w
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
bioRxiv, 2024, 10.1101/2024.01.22.575998
Nat Cell Biol, 2023, 25(7):975-988
Mol Cell, 2023, 83(19):3485-3501.e11
S3592 4-PBA (4-Phenylbutyric acid) 4-PBA (4-Phenylbutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
Int J Biol Sci, 2024, 20(4):1279-1296
Cell Mol Biol Lett, 2023, 28(1):15
PLoS Pathog, 2023, 19(3):e1011295
S1627 Nitazoxanide Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Biomed Pharmacother, 2024, 171:116195
Viruses, 2024, 16(2)282
iScience, 2022, 25(11):105342
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Bone Res, 2022, 10(1):27
Cell Death Dis, 2022, 13(11):1000
iScience, 2022, 25(11):105394
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Cell Cycle, 2022, 1-11.
Aging (Albany NY), 2021, 13(13):17097-17117
S1041 STF-62247 STF-62247 is a molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. STF-62247 shows selective toxicity and growth inhibition of renal cells lacking VHL; 25-fold greater sensitivity observed for cells with VHL deficiency compared to wild-type (VHL+).
Neuropsychiatr Dis Treat, 2015, 11:2091-9
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11

Autophagy阻害剤の選択性比較

Autophagyシグナル伝達経路

Autophagyシグナル伝達経路
Tags: Autophagy inhibitor|Autophagy agonist|Autophagy activator|Autophagy inducer|Autophagy antagonist|Autophagy signaling pathway|Autophagy assay kit