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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S6716	NSC 185058	<1 mg/mL	43 mg/mL	21 mg/mL
S6471	Lucanthone	<1 mg/mL	33 mg/mL	68 mg/mL
S8793	ULK-101	<1 mg/mL	92 mg/mL	<1 mg/mL
S8807	PFK158	˂1 mg/mL	14 mg/mL	4 mg/mL
S8808	DC661	<1 mg/mL	62 mg/mL	49 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
S1105	LY294002	<1 mg/mL	36 mg/mL	21 mg/mL
S1150	Paclitaxel	<1 mg/mL	171 mg/mL	18 mg/mL
S2758	Wortmannin	<1 mg/mL	85 mg/mL	<1 mg/mL
S2767	3-Methyladenine (3-MA)	10 mg/mL	3 mg/mL	4 mg/mL
S2775	Nocodazole	<1 mg/mL	7 mg/mL	<1 mg/mL
S4157	Chloroquine Phosphate	100 mg/mL	<1 mg/mL	<1 mg/mL
S1835	Azithromycin	<1 mg/mL	100 mg/mL	100 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
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
S4430	Hydroxychloroquine Sulfate	67 mg/mL	<1 mg/mL	<1 mg/mL
S7949	MRT68921 HCl	<1 mg/mL	<1 mg/mL	<1 mg/mL
S7683	PIK-III	<1 mg/mL	63 mg/mL	63 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
S9150	Daurisoline	-1 mg/mL	64 mg/mL	-1 mg/mL
S1047	Vorinostat (SAHA, MK0683)	<1 mg/mL	52 mg/mL	3 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
S1039	Rapamycin (Sirolimus)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1023	Erlotinib HCl (OSI-744)	<1 mg/mL	4 mg/mL	<1 mg/mL
S6650	EN6	<1 mg/mL	74 mg/mL	<1 mg/mL
S1057	Obatoclax Mesylate (GX15-070)	<1 mg/mL	83 mg/mL	<1 mg/mL
S1038	PI-103	<1 mg/mL	24 mg/mL	<1 mg/mL
S1149	Gemcitabine HCl	19 mg/mL	<1 mg/mL	<1 mg/mL
S2218	Torkinib (PP242)	<1 mg/mL	61 mg/mL	18 mg/mL
S1237	Temozolomide	<1 mg/mL	38 mg/mL	<1 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
S1972	Tamoxifen Citrate	<1 mg/mL	100 mg/mL	100 mg/mL
S2827	Torin 1	<1 mg/mL	2 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
S1714	Gemcitabine	52 mg/mL	52 mg/mL	<1 mg/mL
S7046	Brefeldin A	<1 mg/mL	4 mg/mL	<1 mg/mL
S2713	Geldanamycin	<1 mg/mL	36 mg/mL	<1 mg/mL
S2929	Pifithrin-α (PFTα) HBr	<1 mg/mL	67 mg/mL	<1 mg/mL
S3030	Niclosamide	<1 mg/mL	<1 mg/mL	<1 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
S3124	Dexamethasone Acetate	<1 mg/mL	87 mg/mL	20 mg/mL
S2491	Nitrendipine	<1 mg/mL	72 mg/mL	<1 mg/mL
S5312	Urolithin A	<1 mg/mL	45 mg/mL	<1 mg/mL
S8595	Tat-beclin 1 (Tat-BECN1)	100 mg/mL	-1 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
S8240	SMER28	<1 mg/mL	52 mg/mL	52 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
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
S4750	Sulfacetamide sodium salt hydrate	50 mg/mL	50 mg/mL	2 mg/mL

Autophagy製品

All (75) Autophagy阻害剤(30) Autophagy活性剤(40) Autophagy作動薬(1) Autophagyモジュレータ(3) Autophagy化学物質(1) 新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
S6716^新	NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
S6471^新	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.
S8793^新	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.
S8807^新	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.
S8808^新	DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).
S8744^新	PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S5920^新	CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
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 in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.	J Ethnopharmacol, 2020, 246:112218 Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
S1150	Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.	Nat Med, 2019, 25(5):838-849 Cancer Discov, 2019, 9(2):230-247 Cancer Cell, 2019, 36(2):179-193	Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm.
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. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.	Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237 Adv Sci (Weinh), 2019, 6(8):1801233	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
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.	J Cell Physiol, 2020, 235(2):1531-1542 Biomed Pharmacother, 2020, 121:109139 Toxicol In Vitro, 2020, 62:104715	granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. P < 0.05 (*P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
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.	Nat Commun, 2019, 10(1):620 Nucleic Acids Res, 2019, 10.1093/nar/gkz602 EMBO J, 2019, 10.15252/embj.2019101863	A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively.
S4157	Chloroquine Phosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.	Sci Adv, 2019, 5(10):eaax7142 EMBO Mol Med, 2019, 11(10):e9930 Theranostics, 2019, 9(26):8392-8408	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.
S1835	Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
S7289	PFK15 PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.	Biochem Biophys Res Commun, 2019, 515(2):332-338 Nat Commun, 2018, 9(1):508 Oncogene, 2018, 37(21):2837-2849	b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays.
S7885	SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.	Elife, 2018, 10.7554/eLife.42253 J Biol Chem, 2018, 293(41):15962-15976 Biochim Biophys Acta, 2017, 1863(11):2796-2807	Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, p < 0.01, * p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05.
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.	Autophagy, 2019, 15(2):312-326 Autophagy, 2019, 10.1080/15548627.2019.1628536 Cancer Lett, 2019, 452:191-202	Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
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.	Autophagy, 2019, 15(3):493-509 Autophagy, 2019, 10.1080/15548627.2019.1606647 Autophagy, 2019, 15(3):493-509	Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; *P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; P < 0.05 vs. I+Exo-124 group.
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.	Cell Rep, 2019, 27(12):3413-3421
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.
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.	Nat Med, 2019, 25(4):628-640 Adv Sci (Weinh), 2019, 6(8):1801233 Nat Commun, 2019, 10(1):2071	C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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.	Nat Cell Biol, 2019, 21(3):372-383 Mol Cell, 2019, 74(2):347-362.e6 Autophagy, 2019, 10.1080/15548627.2019.1686729
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.	EMBO J, 2019, 38(8):e100312 EMBO J, 2019, 38(8):e100312 Cancer Lett, 2018, 435:32-43	LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm
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.
S9150	Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.	Cell, 2019, 176(1-2):198-212 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype).
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. Phase 2.	Mol Cell, 2019, 74(1):19-31 Nat Commun, 2019, 10(1):5770 EMBO J, 2019, 38(11)	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1049	Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with K_i of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.	Cell, 2019, 179(1):147-164 Cell, 2019, 176(5):1158-1173 Nat Genet, 2019, 51(6):999-1010	The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.	Nat Commun, 2020, 11(1):37 Biomed Pharmacother, 2020, 121:109139 Cell, 2019, 176(6):1379-1392	H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) 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.	Cell, 2019, 178(4):807-819.e21 Nat Immunol, 2019, 20(7):835-851 Gastroenterology, 2019, 156(6):1788-1804	Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone.
S6650^新	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.
S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.	Cancer Cell, 2019, 36(1):68-83 Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011 Int J Mol Sci, 2019, 20(6)	In vivo antitumor efﬁcacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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.	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Gastroenterology, 2019, 157(6):1615-1629	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
S1149	Gemcitabine HCl Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.	Cancer Cell, 2019, 35(3):519-533 J Immunother Cancer, 2019, 7(1):199 J Control Release, 2019, 305:89-100	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
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.	Acta Neuropathol, 2019, 138(1):67-84 Acta Neuropathol, 2019, 138(1):67-84 Mol Cell, 2019, 73(4):830-844	Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs^+24/44/ESA viability. CSCs^+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.
S1237	Temozolomide Temozolomide is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells.	Nat Commun, 2019, 10(1):4529 J Pineal Res, 2019, 66(3):e12556 Autophagy, 2019, 15(6):1100-1111	C57BL/6 mice were implanted in the striatum with citrine-GL26-Cherry-HMGB1, which were stably transfected to express the YFP citrine and HMGB1 fused to red fluorescent protein cherry. Fourteen days later, they were treated with saline, Ad-TK+Ad-Flt3L, or Ad-TK+Ad-Flt3L+TMZ (temozolomide). Five days after treatment, the cellular location of cherry-HMGB1 in these cells was assessed by confocal microscopy. Arrows, tumor cells (green) with cytoplasmic HMGB1 (red).
S1950	Metformin HCl Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).	Biomed Pharmacother, 2019, 109:2548-2560 Cancer Med, 2019, 10.1002/cam4.2723 Biochem Biophys Res Commun, 2019, 515(2):332-338	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077), 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.	Nat Commun, 2020, 11(1):71 Gastroenterology, 2019, 10.1053/j Sci Signal, 2019, 12(587)	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1972	Tamoxifen Citrate Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.	Cell Chem Biol, 2019, 26(3):420-432 University of North Texas, 2014, Timothy E. Richardson	Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.
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.	Cell, 2019, 177(4):896-909 Mol Cell, 2019, 73(4):788-802 Mol Cell, 2019, 73(4):788-802	Huh-7.5 cells were treated with increasing concentration of Torin 1, a known autophagy inducer, and the autophagy response was assessed by measuring LC3II and p62 levels.
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.	Free Radic Biol Med, 2019, 147:212-219 Rheumatology (Oxford), 2019, 10.1093/rheumatology/kez165 J Cell Mol Med, 2019, 23(4):2702-2710	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
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.	Cancer Discov, 2019, 9(5):628-645 Clin Cancer Res, 2019, 10.1158/1078-0432 Mol Ther, 2019, 10.1016/j.ymthe.2019.08.011	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S1714	Gemcitabine Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy.	Nat Med, 2019, 25(5):838-849 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0206 Cancer Res, 2019, 79(8):2009-2020	RNA incorporating drugs induce SG assembly. HeLa cells were treated with the RNA incorporating agents 5-azacytidine (50 uM) and 6-thioguanine (10 uM), or the DNA incorporating agents trifluorothymidine (10 uM) and gemcitabine (100 nM) for 72 h. Subsequently, the cellular localization of the SG marker protein TIAR (green) and the P-body marker protein DCP1 (red) was analyzed. Nuclei were stained with Hoechst. Scale bars represent 20 um.
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.	Nat Microbiol, 2019, 4(5):813-825 EMBO J, 2019, 38(8) Cells, 2019, 8(3)	Cells were treated with brefeldin A or manumycin A, and the resulting supernatant was collected after 48 h for exosomal preparation (lanes 1 and 2), or exosomes obtained from C81 cells were trypsin-treated or freeze/thawed (F/T) and then trypsin-treated (lanes 3 and 4). Lanes 5 and 6, input exosome controls from C81 or CEM cells, respectively. Resulting exosomes were assayed for the presence of Tax by Western blotting.
S2713	Geldanamycin Geldanamycin is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.	Nat Commun, 2019, 10(1):2131 Autophagy, 2019, 15(9):1558-1571 Autophagy, 2019, 15(9):1558-1571	Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.	Mol Cell, 2019, S1097-2765(19)30838-X Redox Biol, 2019, 22:101157 Stem Cell Res Ther, 2019, 10(1):123	A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
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).	Nat Microbiol, 2019, 4(5):813-825 J Immunother Cancer, 2019, 7(1):245 Oncol Rep, 2019, 41(4):2389-2395	Effects of some confirmed hits on IRF7 transcription level in response to IFN-α2a treatment (1 h) in SH-SY5Y cells. Data represent mean expression fold±SEM relative to GAPDH, measured from three independent experiments, each in triplicates. P<0.05, P<0.01, and **P<0.001 compared to IFN-α2a treated cells.
S1389	Omeprazole Omeprazole is a proton pump inhibitor, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.
S1979	Amiodarone HCl Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.	Cell Syst, 2019, 8(2):97-108 Gynecol Oncol, 2018, 151(3):525-532 Toxicol Appl Pharmacol, 2015, 285(1):51-60	Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. P<0.05, P<0.01, and **P<0.0001.
S2480	Loperamide HCl Loperamide HCl is a selective μ-opioid receptor agonist opioid with K_i 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.	Exp Ther Med, 2019, 17(2):1312-1320 Neurogastroenterol Motil, 2016, 28(8):1241-51 Antimicrob Agents Chemother, 2014, 58(8):4875-84	Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
S4028	Dexamethasone Sodium Phosphate 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.	Nat Commun, 2015, 6:8481	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S1693	Carbamazepine Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.	DNA Cell Biol, 2019, 10.1089/dna.2018.4553
S2458	Clonidine HCl Clonidine HCl is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg.
S1837	Flubendazole Flubendazole is an autophagy inducer by targeting Atg4B, used to treat internal parasite and worm infection.	RSC Advances, 2018, 10.1039/C7RA12259D	Inhibitory curves and IC50 values for the reference compound flubendazole (B) against VEGFR2.
S1747	Nimodipine Nimodipine is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.	Antiviral Res, 2016, 132:38-45	Assessment of the role of Ca2+ channels during RSV replication. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with calcium channel blockers nifedipine, nimodipine, and tetrandrine (A), at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. NS, no differences at a significance level of 0.05.
S3124	Dexamethasone Acetate 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.	Neuroscience, 2018, 390:151-159 Nat Commun, 2015, 6:8481	Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments.
S2491	Nitrendipine Nitrendipine is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
S5312	Urolithin A Urolithin A, a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption.
S8595	Tat-beclin 1 (Tat-BECN1) Tat-beclin 1 (Tat-BECN1), a peptide known to stimulate autophagy through mobilization of endogenous Beclin 1, induces autophagy in vitro and in vivo and improves clinical outcomes.	Int J Biol Sci, 2019, 15(4):882-894 Mol Carcinog, 2019, 10.1002/mc.23050
S3653	Spermidine trihydrochloride Spermidine, 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).
S9027	Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S4081	Sulfacetamide Sodium Sulfacetamide Sodium is an anti-biotic.
S8240	SMER28 SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.	Cell Rep, 2019, 27(12):3413-3421 Cells, 2019, 8(4) Cell Biochem Biophys, 2011, 60(3):173-85
S9310	Isorhychophylline Isorhynchophylline 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.
S1238	Tamoxifen Tamoxifen is an antagonist of the estrogen receptor in breast tissue.	Exp Cell Res, 2020, 386(1):111713 Mol Cell, 2019, 75(6):1103-1116.e9 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-18-4044	E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01.
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.	Exp Eye Res, 2019, 184:126-134
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.	Cancer Lett, 2020, 469:111-123 Cancer Discov, 2019, 9(2):230-247 Cancer Res, 2019, 79(20):5382-5393	for HXO-RB44 cells, IC50 values for VCR were changed in the different SG600 treatment groups. The results are representative of three independent experiments and of f our replicates in each experiment.
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.	Mol Cancer Ther, 2019, 18(5):900-908 Front Oncol, 2019, 9:579 Cancer Biol Ther, 2018, 19(9):797-808	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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	Columns depict relative densitometric values that were obtained by comparing with (β-actin. Presenilin 1, Nicastrin, and Pen-2 were increased with the 3-MA treatment (P<0.001) while the other component of the γ-secretase complex (APH-1 and Presenilin 2) has no difference, compared with the STF-62247 treatment. Moreover, Bace1 and ADAM17 respectively had no difference between 3-MA and STF-62247 treatments. Both autophagy inhibitor and inducer activated α-, β-, and γ-secretases (P<0.005). Abbreviations: Aβ, beta-amyloid; ADAM17, a disintegrin and metalloprotease 17; APH-1, anterior pharynx-defective 1; APP, amyloid protein precursor; Bace1, beta-site APP cleavage enzyme; 3-MA, 3-methyladenine; Con, control, LC3, microtubule-associated protein 1A/1B-light chain 3.
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.

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S6716^新	NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
S6471^新	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.
S8793^新	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.
S8807^新	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.
S8808^新	DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).
S8744^新	PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S5920^新	CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
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 in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.	J Ethnopharmacol, 2020, 246:112218 Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237	Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
S1150	Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.	Nat Med, 2019, 25(5):838-849 Cancer Discov, 2019, 9(2):230-247 Cancer Cell, 2019, 36(2):179-193	Microscope image (406) magnification of U937 cells after exposure to SM-TNs. a) Untreated U937 cells. b) U937 cells treated with 200 nM, and 35 nM ODS empty shells. c) U937 cells treated with microcrystalline (free) Taxol prepared by sonicating Taxol in 20%H3PO4/0.8% SDS solution. d) U937 cells treated with 200 nM SM-TN. A SM-TN is seen in the middle of the picture. e) U937 cells treated with 35 nM SMTN.The nanowires are too small to see at this magnification, but their effect on the cells is clearly visible. Scale bar = 10 mm.
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. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.	Cell, 2019, 176(6):1379-1392 Nat Cell Biol, 2019, 21(2):226-237 Adv Sci (Weinh), 2019, 6(8):1801233	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
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.	J Cell Physiol, 2020, 235(2):1531-1542 Biomed Pharmacother, 2020, 121:109139 Toxicol In Vitro, 2020, 62:104715	granulosa cells (GCs) with 24 h of melatonin (10 μM) treatment were rinsed in PBS, and then exposed to H2O2 (200 μM) for 2 h. The autophagy inhibitor 3-MA (10 mM), or the apoptosis inhibitor Z-VAD-FMK (50 μM) were added 1 h prior to H2O2 incubation. Cell viability was determined using the CCK-8 assay. Data represent mean ± S.E; n = 3 in each group. P < 0.05 (*P < 0.01) vs. vehicle group at 0 h. # Represents P < 0.05 (## Represents P < 0.01) vs. H2O2-only-treated cells. & Represents P > 0.05 vs. H2O2-only-treated cells. N, not significant, P > 0.05. δ Represents P < 0.05 (δδ Represents P < 0.01) vs. Z-VAD-FMK-treated cells.
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.	Nat Commun, 2019, 10(1):620 Nucleic Acids Res, 2019, 10.1093/nar/gkz602 EMBO J, 2019, 10.15252/embj.2019101863	A, HeLa cells were treated with DMSO, Taxol (100 nM for 16 h), or Nocodazole (Noco, 100 ng/ml for 16 h). Total cell lysates were probed with the indicated antibodies against Hippo components on Phos-tag SDS-polyacrylamide gels. O and * mark the non-phosphorylated and phosphorylated proteins, respectively.
S4157	Chloroquine Phosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.	Sci Adv, 2019, 5(10):eaax7142 EMBO Mol Med, 2019, 11(10):e9930 Theranostics, 2019, 9(26):8392-8408	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.
S1835	Azithromycin Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
S7289	PFK15 PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.	Biochem Biophys Res Commun, 2019, 515(2):332-338 Nat Commun, 2018, 9(1):508 Oncogene, 2018, 37(21):2837-2849	b EdU incorporation assays indicated PFK15 inhibited the cell proliferation of Cal27 cells. c The quantitative data of the EdU incorporation assays.
S7885	SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.	Elife, 2018, 10.7554/eLife.42253 J Biol Chem, 2018, 293(41):15962-15976 Biochim Biophys Acta, 2017, 1863(11):2796-2807	Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, p < 0.01, * p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05.
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.	Autophagy, 2019, 15(2):312-326 Autophagy, 2019, 10.1080/15548627.2019.1628536 Cancer Lett, 2019, 452:191-202	Western blot analyses show significant inhibition of autophagy-related gene expression in Spautin-1 treated OCI-AML2 cells after Ara-C treatment.
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.	Autophagy, 2019, 15(3):493-509 Autophagy, 2019, 10.1080/15548627.2019.1606647 Autophagy, 2019, 15(3):493-509	Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; *P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; P < 0.05 vs. I+Exo-124 group.
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.	Cell Rep, 2019, 27(12):3413-3421
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.
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.	Nat Med, 2019, 25(4):628-640 Adv Sci (Weinh), 2019, 6(8):1801233 Nat Commun, 2019, 10(1):2071	C, SA-beta gal staining results of A549-LKB1 cells treated by trametinib (30 nmol/L), radiotherapy (2 Gy), and HCQ (50 μmol/L). Cells were treated by HCQ and/or trametinib 4 hours prior to radiotherapy. Drugs were washed out 24 hours after radiotherapy. Cells were incubated for additional 48 hours before staining. D, Clonogenic survival assay of A549-LKB1 cells treated with trametinib (30 nmol/L) and HCQ (50 μmol/L).
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.	Nat Cell Biol, 2019, 21(3):372-383 Mol Cell, 2019, 74(2):347-362.e6 Autophagy, 2019, 10.1080/15548627.2019.1686729
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.	EMBO J, 2019, 38(8):e100312 EMBO J, 2019, 38(8):e100312 Cancer Lett, 2018, 435:32-43	LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm
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.
S9150	Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.

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S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.	Cell, 2019, 176(1-2):198-212 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype).
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. Phase 2.	Mol Cell, 2019, 74(1):19-31 Nat Commun, 2019, 10(1):5770 EMBO J, 2019, 38(11)	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1049	Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with K_i of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.	Cell, 2019, 179(1):147-164 Cell, 2019, 176(5):1158-1173 Nat Genet, 2019, 51(6):999-1010	The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.	Nat Commun, 2020, 11(1):37 Biomed Pharmacother, 2020, 121:109139 Cell, 2019, 176(6):1379-1392	H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.
S1023	Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) 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.	Cell, 2019, 178(4):807-819.e21 Nat Immunol, 2019, 20(7):835-851 Gastroenterology, 2019, 156(6):1788-1804

研究分野別

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Autophagy

シグナル伝達経路

研究分野

阻害剤の選択性比較

Autophagy製品