Autophagy

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1013 Bortezomib (PS-341) <1 mg/mL 76 mg/mL <1 mg/mL
S6851 RA-190 <1 mg/mL 100 mg/mL '20 mg/mL
S8943 VLX600 ˂1 mg/mL 13 mg/mL ˂1 mg/mL
S6716 NSC 185058 <1 mg/mL 43 mg/mL 21 mg/mL
S7455 Resatorvid (TAK-242) <1 mg/mL 72 mg/mL '72 mg/mL
S1109 BI 2536 <1 mg/mL 21 mg/mL '100 mg/mL
S1105 LY294002 <1 mg/mL 36 mg/mL 21 mg/mL
S1092 KU-55933 (ATM Kinase Inhibitor) <1 mg/mL 33 mg/mL ''<1 mg/mL
S1102 U0126-EtOH <1 mg/mL 85 mg/mL ''<1 mg/mL
S1150 Paclitaxel <1 mg/mL 171 mg/mL '18 mg/mL
S1460 SP600125 <1 mg/mL 44 mg/mL '<1 mg/mL
S1490 Ponatinib (AP24534) <1 mg/mL 30 mg/mL '<1 mg/mL
S1113 GSK690693 <1 mg/mL 39 mg/mL ''<1 mg/mL
S2758 Wortmannin <1 mg/mL 85 mg/mL '<1 mg/mL
S2704 LY2109761 <1 mg/mL 2 mg/mL '<1 mg/mL
S2767 3-Methyladenine (3-MA) 10 mg/mL 3 mg/mL '4 mg/mL
S2243 Degrasyn (WP1130) <1 mg/mL 77 mg/mL '18 mg/mL
S1786 Verteporfin <1 mg/mL 100 mg/mL ''<1 mg/mL
S7046 Brefeldin A <1 mg/mL 4 mg/mL '<1 mg/mL
S8037 Necrostatin-1 <1 mg/mL 51 mg/mL ''<1 mg/mL
S2775 Nocodazole <1 mg/mL 7 mg/mL <1 mg/mL
S3042 Purmorphamine <1 mg/mL 4 mg/mL '<1 mg/mL
S4157 Chloroquine Phosphate 100 mg/mL <1 mg/mL '''<1 mg/mL
S1413 Bafilomycin A1(Baf-A1) <1 mg/mL 6 mg/mL '<1 mg/mL
S1835 Azithromycin <1 mg/mL 100 mg/mL '100 mg/mL
S8808 DC661 <1 mg/mL 62 mg/mL '49 mg/mL
S7289 PFK15 <1 mg/mL 19 mg/mL 2 mg/mL
S7885 SBI-0206965 <1 mg/mL 97 mg/mL '10 mg/mL
S8576 EAD1 100 mg/mL 100 mg/mL 100 mg/mL
S8764 IITZ-01 <1 mg/mL 100 mg/mL <1 mg/mL
S7888 Spautin-1 <1 mg/mL 54 mg/mL ''7 mg/mL
S8317 3BDO <1 mg/mL 65 mg/mL '49 mg/mL
S7811 MHY1485 <1 mg/mL 4 mg/mL <1 mg/mL
S8596 Autophinib <1 mg/mL 69 mg/mL <1 mg/mL
S7423 KN-93 Phosphate 92 mg/mL 100 mg/mL '<1 mg/mL
S8807 PFK158 ˂1 mg/mL 14 mg/mL 4 mg/mL
S3758 Cucoline hydrochloride, Kukoline hydrochloride, Sabianine A hydrochloride -1 mg/mL 73 mg/mL -1 mg/mL
S8369 Lys05 3 mg/mL 9 mg/mL <1 mg/mL
S7660 Obeticholic Acid <1 mg/mL 84 mg/mL '84 mg/mL
S4430 Hydroxychloroquine Sulfate 67 mg/mL <1 mg/mL '<1 mg/mL
S7949 MRT68921 HCl <1 mg/mL <1 mg/mL '<1 mg/mL
S8744 PHY34 <1 mg/mL 100 mg/mL 42 mg/mL
S5920 CA-5f <1 mg/mL 78 mg/mL <1 mg/mL
S7683 PIK-III <1 mg/mL 63 mg/mL 63 mg/mL
S8793 ULK-101 <1 mg/mL 92 mg/mL '''<1 mg/mL
S8527 ROC-325 <1 mg/mL 4 mg/mL 4 mg/mL
S9424 Liensinine diperchlorate -1 mg/mL 50 mg/mL -1 mg/mL
S6471 Lucanthone <1 mg/mL 33 mg/mL 68 mg/mL
S9150 Daurisoline -1 mg/mL 64 mg/mL -1 mg/mL
S1078 MK-2206 2HCl <1 mg/mL 14 mg/mL <1 mg/mL
S1060 Olaparib (AZD2281) 0.002 mg/mL 86 mg/mL <1 mg/mL
S1267 Vemurafenib (PLX4032) <1 mg/mL 97 mg/mL <1 mg/mL
S1047 Vorinostat (SAHA) <1 mg/mL 52 mg/mL '3 mg/mL
S6797 QX77 <1 mg/mL 60 mg/mL <1 mg/mL
S6650 EN6 <1 mg/mL 74 mg/mL <1 mg/mL
S1002 ABT-737 <1 mg/mL 100 mg/mL '<1 mg/mL
S1049 Y-27632 2HCl 14 mg/mL 64 mg/mL '<1 mg/mL
S2619 MG-132 <1 mg/mL 90 mg/mL 25 mg/mL
S1009 Dactolisib (BEZ235) <1 mg/mL 0.01 mg/mL '<1 mg/mL
S1040 Sorafenib Tosylate 0.01 mg/mL 127 mg/mL '''<1 mg/mL
S1021 Dasatinib <1 mg/mL 98 mg/mL <1 mg/mL
S1039 Rapamycin (Sirolimus) <1 mg/mL 20 mg/mL '<1 mg/mL
S1068 Crizotinib (PF-02341066) <1 mg/mL 9 mg/mL '<1 mg/mL
S1023 Erlotinib HCl (OSI-744) <1 mg/mL 4 mg/mL <1 mg/mL
S1120 Everolimus (RAD001) <1 mg/mL 100 mg/mL 7 mg/mL
S1025 Gefitinib (ZD1839) <1 mg/mL 89 mg/mL 4 mg/mL
S1004 Veliparib (ABT-888) <1 mg/mL 17 mg/mL ''<1 mg/mL
S1053 Entinostat (MS-275) <1 mg/mL 75 mg/mL '<1 mg/mL
S1065 Pictilisib (GDC-0941) <1 mg/mL 44 mg/mL '<1 mg/mL
S1378 Ruxolitinib (INCB018424) <1 mg/mL 61 mg/mL 61 mg/mL
S1030 Panobinostat (LBH589) <1 mg/mL 69 mg/mL '<1 mg/mL
S1026 Imatinib Mesylate (STI571) 118 mg/mL 118 mg/mL ''<1 mg/mL
S1250 Enzalutamide (MDV3100) <1 mg/mL 92 mg/mL '<1 mg/mL
S1133 Alisertib (MLN8237) <1 mg/mL 27 mg/mL <1 mg/mL
S1011 Afatinib (BIBW2992) <1 mg/mL 97 mg/mL 15 mg/mL
S2226 Idelalisib (CAL-101, GS-1101) <1 mg/mL 83 mg/mL '23 mg/mL
S1048 Tozasertib (VX-680, MK-0457) <1 mg/mL 93 mg/mL '<1 mg/mL
S1555 zad8555 <1 mg/mL 50 mg/mL '3 mg/mL
S1006 Saracatinib (AZD0530) <1 mg/mL 35 mg/mL '31 mg/mL
S1057 Obatoclax Mesylate (GX15-070) <1 mg/mL 83 mg/mL <1 mg/mL
S1141 Tanespimycin (17-AAG) <1 mg/mL 100 mg/mL '5 mg/mL
S1166 Cisplatin <1 mg/mL 60 mg/mL ''<1 mg/mL
S1033 Nilotinib (AMN-107) <1 mg/mL 27 mg/mL '<1 mg/mL
S1044 Temsirolimus (CCI-779) <1 mg/mL 67 mg/mL '75 mg/mL
S1038 PI-103 <1 mg/mL 24 mg/mL '<1 mg/mL
S1069 Luminespib (NVP-AUY922) <1 mg/mL 93 mg/mL ''31 mg/mL
S1149 Gemcitabine HCl 19 mg/mL <1 mg/mL ''<1 mg/mL
S1122 Mocetinostat (MGCD0103) <1 mg/mL 13 mg/mL '<1 mg/mL
S1178 Regorafenib (BAY 73-4506) <1 mg/mL 97 mg/mL ''<1 mg/mL
S1129 SRT1720 HCl <1 mg/mL 38 mg/mL '<1 mg/mL
S1014 Bosutinib (SKI-606) <1 mg/mL 100 mg/mL ''''2 mg/mL
S1077 SB202190 (FHPI) <1 mg/mL 66 mg/mL '12 mg/mL
S2853 Carfilzomib (PR-171) <1 mg/mL 50 mg/mL ''<1 mg/mL
S1191 Fulvestrant <1 mg/mL 100 mg/mL '100 mg/mL
S1075 SB216763 <1 mg/mL 23 mg/mL ''<1 mg/mL
S1135 Pemetrexed 94 mg/mL <1 mg/mL <1 mg/mL
S2218 Torkinib (PP242) <1 mg/mL 61 mg/mL 18 mg/mL
S1225 Etoposide <1 mg/mL 100 mg/mL '''<1 mg/mL
S2248 Silmitasertib (CX-4945) <1 mg/mL 16 mg/mL '<1 mg/mL
S8048 Venetoclax (ABT-199) <1 mg/mL 100 mg/mL <1 mg/mL
S1230 Flavopiridol (Alvocidib) <1 mg/mL 15 mg/mL 8 mg/mL
S2111 Lapatinib <1 mg/mL 100 mg/mL '<1 mg/mL
S1237 Temozolomide <1 mg/mL 38 mg/mL <1 mg/mL
S5003 Tacrolimus (FK506) <1 mg/mL 94 mg/mL ''83 mg/mL
S1950 Metformin HCl 33 mg/mL <1 mg/mL '<1 mg/mL
S1573 Fasudil (HA-1077) HCl 65 mg/mL 5 mg/mL '<1 mg/mL
S1224 Oxaliplatin 3 mg/mL -1 mg/mL '''0.01 mg/mL
S7110 (+)-JQ1 <1 mg/mL 91 mg/mL 91 mg/mL
S2181 Ixazomib Citrate (MLN9708) <1 mg/mL 100 mg/mL '<1 mg/mL
S1972 Tamoxifen Citrate <1 mg/mL 100 mg/mL 100 mg/mL
S2827 Torin 1 <1 mg/mL 2 mg/mL <1 mg/mL
S2658 Omipalisib (GSK2126458) <1 mg/mL 100 mg/mL '<1 mg/mL
S1782 Azacitidine (5-Azacytidine) <1 mg/mL 48 mg/mL ''<1 mg/mL
S2180 Ixazomib (MLN2238) <1 mg/mL 72 mg/mL ''9 mg/mL
S1590 TWS119 <1 mg/mL 64 mg/mL '<1 mg/mL
S1396 Resveratrol <1 mg/mL 45 mg/mL <1 mg/mL
S1322 Dexamethasone <1 mg/mL 79 mg/mL '''6 mg/mL
S1648 Cytarabine 48 mg/mL 1 mg/mL ''''<1 mg/mL
S1792 Simvastatin <1 mg/mL 83 mg/mL '83 mg/mL
S1714 Gemcitabine 52 mg/mL 52 mg/mL '<1 mg/mL
S2163 PF-4708671 <1 mg/mL 30 mg/mL 8 mg/mL
S2817 Torin 2 <1 mg/mL 20 mg/mL ''''<1 mg/mL
S1582 H 89 2HCl 6 mg/mL 104 mg/mL '<1 mg/mL
S2713 Geldanamycin <1 mg/mL 36 mg/mL <1 mg/mL
S2770 MK-5108 (VX-689) <1 mg/mL 92 mg/mL '<1 mg/mL
S2449 Forskolin <1 mg/mL 82 mg/mL '37 mg/mL
S7306 Dorsomorphin (Compound C) 2HCl 94 mg/mL <1 mg/mL '<1 mg/mL
S2505 Rosiglitazone maleate <1 mg/mL 94 mg/mL '<1 mg/mL
S2799 Daporinad (FK866, APO866) <1 mg/mL <1 mg/mL '78 mg/mL
S2929 Pifithrin-α (PFTα) HBr <1 mg/mL 67 mg/mL '<1 mg/mL
S7164 GSK343 <1 mg/mL 1 mg/mL '4 mg/mL
S8059 Nutlin-3a <1 mg/mL 100 mg/mL '100 mg/mL
S7007 Binimetinib (MEK162) <1 mg/mL 88 mg/mL '<1 mg/mL
S2751 Milciclib (PHA-848125) <1 mg/mL 92 mg/mL '<1 mg/mL
S7397 Sorafenib <1 mg/mL 63 mg/mL '''''<1 mg/mL
S2556 Rosiglitazone <1 mg/mL 71 mg/mL '<1 mg/mL
S3030 Niclosamide <1 mg/mL <1 mg/mL <1 mg/mL
S8047 Dynasore <1 mg/mL 64 mg/mL '<1 mg/mL
S1263 CHIR-99021 (CT99021) <1 mg/mL 10 mg/mL <1 mg/mL
S8075 GANT61 <1 mg/mL <1 mg/mL '12 mg/mL
S1389 Omeprazole <1 mg/mL 69 mg/mL 13 mg/mL
S1979 Amiodarone HCl <1 mg/mL 23 mg/mL 11 mg/mL
S2480 Loperamide HCl <1 mg/mL 22 mg/mL 4 mg/mL
S4028 Dexamethasone Sodium Phosphate 103 mg/mL <1 mg/mL <1 mg/mL
S1693 Carbamazepine <1 mg/mL 47 mg/mL 18 mg/mL
S2458 Clonidine HCl 53 mg/mL 53 mg/mL 53 mg/mL
S1837 Flubendazole <1 mg/mL 3 mg/mL <1 mg/mL
S1747 Nimodipine <1 mg/mL 84 mg/mL 84 mg/mL
S7067 Tepotinib (EMD 1214063) <1 mg/mL 5 mg/mL '<1 mg/mL
S7177 PF-543 <1 mg/mL 93 mg/mL ''93 mg/mL
S2491 Nitrendipine <1 mg/mL 72 mg/mL <1 mg/mL
S5243 Ruxolitinib Phosphate 29 mg/mL 80 mg/mL '8 mg/mL
S7781 Sunitinib <1 mg/mL 25 mg/mL ''<1 mg/mL
S7786 Erlotinib <1 mg/mL 78 mg/mL '15 mg/mL
S8595 Tat-beclin 1 (Tat-BECN1) 100 mg/mL -1 mg/mL -1 mg/mL
S5715 atorvastatin -1 mg/mL 100 mg/mL '-1 mg/mL
S7655 CB-839 <1 mg/mL 100 mg/mL <1 mg/mL
S3653 Spermidine trihydrochloride 50 mg/mL 30 mg/mL <1 mg/mL
S9027 Corynoxine <1 mg/mL 77 mg/mL 77 mg/mL
S4081 Sulfacetamide Sodium 51 mg/mL 19 mg/mL <1 mg/mL
S7483 DMOG 35 mg/mL 35 mg/mL '35 mg/mL
S8240 SMER28 <1 mg/mL 52 mg/mL 52 mg/mL
S7104 AZD1208 <1 mg/mL 75 mg/mL ''<1 mg/mL
S4546 Xylitol 30 mg/mL 30 mg/mL <1 mg/mL
S7840 Dorsomorphin (Compound C, BML-275) <1 mg/mL 1 mg/mL '2 mg/mL
S9310 Isorhychophylline -1 mg/mL 77 mg/mL -1 mg/mL
S1238 Tamoxifen <1 mg/mL 74 mg/mL ''74 mg/mL
S8597 LYN-1604 100 mg/mL 50 mg/mL '100 mg/mL
S2924 CHIR-99021 (CT99021) HCl <1 mg/mL 93 mg/mL 2 mg/mL
S2215 DAPT (GSI-IX) <1 mg/mL 86 mg/mL 50 mg/mL
S1241 Vincristine sulfate 60 mg/mL 100 mg/mL ''<1 mg/mL
S1168 Valproic acid sodium salt (Sodium valproate) 33 mg/mL 33 mg/mL 33 mg/mL
S1041 STF-62247 <1 mg/mL 53 mg/mL 3 mg/mL
S7153 10058-F4 <1 mg/mL 49 mg/mL '4 mg/mL
S7980 VPS34-IN1 <1 mg/mL 85 mg/mL ''85 mg/mL
S4750 Sulfacetamide sodium salt hydrate 50 mg/mL 50 mg/mL 2 mg/mL

Autophagy製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1013

Bortezomib (PS-341)

Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

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.

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.

S6716

NSC 185058

NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.

S7455

Resatorvid (TAK-242)

Resatorvid (TAK-242) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid inhibits autophagy.

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.

S1105

LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.

S1092

KU-55933 (ATM Kinase Inhibitor)

KU-55933 (ATM Kinase Inhibitor) 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.

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.

S1150

Paclitaxel

Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.

S1460

SP600125

SP600125 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.

S1490

Ponatinib (AP24534)

Ponatinib (AP24534) 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.

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.

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.

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.

S2767

3-Methyladenine (3-MA)

3-Methyladenine (3-MA) 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. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.

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.

S1786

Verteporfin

Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.

S7046

Brefeldin A

Brefeldin A 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.

S8037

Necrostatin-1

Necrostatin-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.

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.

S3042

Purmorphamine

Purmorphamine, 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.

S4157

Chloroquine Phosphate

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).

S1413

Bafilomycin A1(Baf-A1)

Bafilomycin A1 is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.

S1835

Azithromycin

Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.

S8808

DC661

DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.

S7289

PFK15

PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.

S7885

SBI-0206965

SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.

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.

S8764

IITZ-01

IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.

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.

S8317

3BDO

3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs.

S7811

MHY1485

MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

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.

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.

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.

S3758

Cucoline hydrochloride, Kukoline hydrochloride, Sabianine A hydrochloride

Sinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.

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.

S7660

Obeticholic Acid

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.

S4430

Hydroxychloroquine Sulfate

Hydroxychloroquine 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.

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.

S8744

PHY34

PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.

S5920

CA-5f

CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.

S7683

PIK-III

PIK-III, 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.

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.

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.

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.

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.

S9150

Daurisoline

Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.

S1078

MK-2206 2HCl

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

S1060

Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

S1267

Vemurafenib (PLX4032)

Vemurafenib (PLX4032, RG7204) 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.

S1047

Vorinostat (SAHA)

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.

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.

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.

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.

S1049

Y-27632 2HCl

Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

S2619

MG-132

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.

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.

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.

S1021

Dasatinib

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.