Autophagy

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S8764	IITZ-01	<1 mg/mL	100 mg/mL	<1 mg/mL
S3758	Sinomenine hydrochloride	-1 mg/mL	73 mg/mL	-1 mg/mL
S8576	EAD1	100 mg/mL	100 mg/mL	100 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
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
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
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
S9027	Corynoxine	<1 mg/mL	77 mg/mL	77 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
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 (DHAP)	<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
S3653	Spermidine trihydrochloride	50 mg/mL	30 mg/mL	<1 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
S1238	Tamoxifen	<1 mg/mL	74 mg/mL	74 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 Inhibitors (66)
New Autophagy Products

Catalog No.	Information	Product Use Citations	Product Validations
S8764^New	IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
S9424^New	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^New	Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
S3758^New	Sinomenine hydrochloride Sinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
S8576^New	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.
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.	Nature, 2015, 10.1038/nature14412 Am J Respir Crit Care Med, 2015, 10.1164/rccm.201501-0188OC Blood, 2014, 123(2):239-48	Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).
S1150	Paclitaxel Paclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.	Science, 2017, eaal3755 Sci Transl Med, 2018, 10(433) Nat Chem Biol, 2016, 10.1038/nchembio.2082	(F) Kaplan-Meier curves are shown for all groups described: no hydrogel, a hydrogel loaded with paclitaxel, or a hydrogel loaded with doxorubicin. The number of mice per group (n) and median survival (ms) are listed. The experiment was performed at least three times.
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.	Nature, 2015, 10.1038/nature14412 Science, 2016, 353(6302):929-32 Cancer Res, 2014, 74(10):2846-56	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.	Cell Death Dis, 2016, 7(6):e2247 Cell Physiol Biochem, 2016, 38(6):2401-13 Am J Cancer Res, 2015, 5(1):125-139	MDC-labeled vacuoles were induced by AZD2014 and inhibited by autophagy inhibitor (3-MA). SMMC-7721 cells were treated with AZD2014 or rapamycin at concentrations of 100 and 600 nM, respectively, for 48 hours in the presence or absence of 3-MA, and then stained with MDC. Cells were immediately observed under a confocal microscope. Cells in the control group were treated with DMSO. bars, 20 μm.
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 improves the CRISPR-mediated HDR efficiency and has an additive effect on enhancing precise genome editing.	J Immunol, 2015, 10.4049/jimmunol.1402897 J Biol Chem, 2016, 10.1074/jbc.M116.722751 Cell Signal, 2016, 28(12):1826-1832	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 phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.	Leukemia, 2017, 10.1038/leu.2016.325 Cell Signal, 2016, 28(8):1086-98 Int J Mol Med, 2017, 10.3892/ijmm.2017.3008	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.	Br J Pharmacol, 2017, 174(9):893-908 J Exp Clin Cancer Res, 2017, 10.1186/s13046-016-0481-1 PLoS One, 2016, 11(9):e0163768	RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone
S7885	SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.	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.
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.	Int J Cancer, 2015, 136(11):2717-29 J Hematol Oncol, 2016, 9(1):45	Autophagosomal inhibition was performed in 32D EV, WT CALR, del52, and ins5 expressing cells. The 32D cell lines were treated with the inhibitor spautin-1 for the indicated time. Lysates were prepared, and SDS-PAGE and Western blotting were performed. Antibodies detecting mutated CALR (CALR mut), CALR, LC3I-II, and GAPDH were used for immunostaining. LC3I-II served as control for successful autophagosomal inhibition.
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.	Biochem J, 2017, 474(16):2733-2747 Mol Med Rep, 2016, 14(4):3662-8	MYH1485, an activator of mTOR, reduced LC3II production and inhibited autophagosome formation in PAR2-knockdown cells.
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.
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.	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1489 Cell Death Dis, 2017, 8(1):e2558 Oxid Med Cell Longev, 2017, 8519169	Expression levels of LC3-I and LC3-II were analyzed by western blotting at 80 and 120 min following BBR-SDT with or without 3MA- and hydroxychloroquine-pretreatments. Quantification of the LC3-II/LC3-I ratios are shown (n=3; Po0.05, Po0.01, **Po0.001 versus control, # P<0.05, ##P<0.01 versus BBR-SDT groups)
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.	Methods Enzymol, 2017, 587:391-404
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. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.	Mol Biosyst, 2017, 13(10):1993-2005	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.
S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.	Nature, 2011, 471(7337):235-9 Nat Biotechnol, 2015, 10.1038/nbt.3130 Nat Biotechnol, 2011, 29(3):255-65	Activity of vorinostat in Jurkat and Peer T-ALL cell lines in an MTT cell viability assay. Cells were treated with increasing drug concentrations for 72 h. The data are plotted as the mean % of DMSO-treated control cells against the corresponding drug concentration. The error bars are the standard error. For each drug and cell line, 3-4 independent experiments were performed with 6 replicates at each drug concentration.
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.	Nat Biotechnol, 2011, 29(6):542-6 Nat Med, 2013, 19(11):1478-88 Cell, 2018, 175(2):429-441	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.	Nature, 2018, 557(7704):256-260 Nature, 2016, 532(7597):107-11 Cell, 2018, 174(2):338-349	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.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.	Nature, 2016, 539(7629):437-442 Nat Genet, 2014, 46(4):364-70 Cancer Cell, 2011, 19(6):792-804	Protein blots showing MYC expression in naive and persister cells after 3 d of treatment with 2 uM AKT inhibitor MK-2206 (AKTi) or 10 nM mTOR inhibitor rapamycin (Rapa).
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, 2012, 151(5):937-50 Nat Genet, 2012, 44(8):852-60 Cancer Discov, 2013, 3(12):1404-15	Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers.
S9027^New	Corynoxine Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.
S9310^New	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.
S5312^New	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^New	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.
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.	Nat Chem Biol, 2015, 10.1038/nchembio.1986 Cancer Res, 2012, 72(12):3069-79 Cancer Res, 2011, 71(13):4494-505	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.	Cell, 2013, 153(4):840-54 Leukemia, 2013, 27(3):650-60 Leukemia, 2012, 26(5):927-33	(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
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.	Sci Transl Med, 2015, 7(284):284ra57 Nucleic Acids Res, 2014, 42(10):6436-47 Clin Cancer Res, 2014, 20(12):3187-97	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.	Science, 2016, 353(6302):929-32 Nat Chem Biol, 2013, 9(11):708-14 J Clin Invest, 2015, 10.1172/JCI78018	MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).
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 Med, 2015, 10.1038/nm.3855 Clin Cancer Res, 2017, 23(2):523-535 Clin Cancer Res, 2014, 20(6):1555-65	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).	Cancer Cell, 2014, 26(6):840-50 Luminescence, 2014, 29(1):65-73 Sci Rep, 2017, 7(1):2169	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.	J Clin Invest, 2014, 124(9):3757-66 J Clin Invest, 2014, 124(4):1646-59 Biosens Bioelectron, 2016, 86:508-515	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.	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.	Cancer Discov, 2016, 6(7):727-39 Elife, 2015, 4 Am J Pathol, 2014, 184(1):214-29	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.	Cell Physiol Biochem, 2015, 35(6):2255-2271 Biochim Biophys Acta, 2016, 1859(2):294-305 Molecules, 2014, 19(12):20570-9	PC-9 and A549 cells were treated with 100 nM siRNA against PUMA and 100 nM negative control (NC) siRNA for 12 h, and treated with the indicated concentrations of RV and ERL in combination for an additional 48 h. The knockdown effects on PUMA were confirmed by Western blot analysis.
S1322	Dexamethasone (DHAP) Dexamethasone (DHAP) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.	Oncogene, 2013, 32(10):1316-29 Xenobiotica, 2016, 46(10):948-52	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.	Nature, 2017, 552(7683):116-120 Sci Transl Med, 2015, 7(284):284ra57 Nucleic Acids Res, 2014, 42(10):6436-47	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. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR.	Nanoscale, 2018, 10(18):8796-8805 EBioMedicine, 2018, 36:229-240 EBioMedicine, 2017, 18:188-198	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.	J Antimicrob Chemother, 2015, 10.1093/jac/dku549 Antimicrob Agents Chemother, 2015, 59(8):4727-33 PLoS One, 2015, 10(9):e0138936	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.	Am J Transplant, 2015, 15(12):3095-111 Cell Prolif, 2017, 10.1111/cpr.12319 Int J Biol Sci, 2016, 12(11):1298-1308	(C) Cell viability was measured after TSA and PFTα co-treatment. MG63 were exposed to TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment compared with TSA treatment alone for 24h. Data are presented as means ± S.E.M. from 3 independent experiments. , P < 0.05 vs. MG63 cells without TSA or PFTα treatment; *, P < 0.01 vs. MG 63 cells without TSA or PFTα treatment; &&, P < 0.01 vs. MG63 cells with TSA treatment alone. (D) Flow cytometry analysis of ANXA5 and propidiumiodide staining of MG63 cells with TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment, compared with TSA treatment alone.
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 Immunopharmacol, 2016, 36:199-204 Onco Targets Ther, 2017, 10:1767-1776	Bacterial infection in IPEC-J2 cells. The invasion and attachment of EHECO157:H7 was increased in the IPEC-J2 cells in the presence of 1 μM niclosamide. Data are expressed as the mean ± SEM (n= 6). Differences between groups were determined by paired samples t-test. *P<0.05 compared with the control.
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.	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.	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Neurogastroenterol Motil, 2016, 28(8):1241-51	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.		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.
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.		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 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.		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.
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).
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.
S1238	Tamoxifen Tamoxifen is an antagonist of the estrogen receptor in breast tissue.	Oncotarget, 2015, 6(4):2315-30 University of North Texas, 2014, Timothy E. Richardson	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.
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 Res, 2013, 73(20):6310-22 J Pharmacol Exp Ther, 2014, 350(3):646-56 Int J Mol Sci, 2012, 13(9):10736-49	Plk inhibitor cooperates with chemotherapeutic agents. Conditional patched mutant tumor cells were treated with increasing concentrations of the chemotherapeutic agents vincristine alone or in combination with 10 nMol/L BI-2536. Cells were cultured for 48 hours, pulsed with 3H-Td, and harvested for analysis of 3H-Td incorporation at 66 hours.
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.	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
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.

Choose Your Country or Region

By Signaling Pathways

By product type

Autophagy

Signaling Pathway Map

Research Area