Autophagy
- Inhibitory Selectivity
- Solubility
Catalog No. | Product Name | Solubility(25°C) | ||
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Water | DMSO | Alcohol | ||
S8764 | IITZ-01 | <1 mg/mL | 100 mg/mL | <1 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 |
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 |
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 | Sinomenine 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 |
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 |
S9310 | Isorhychophylline | -1 mg/mL | 77 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 |
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 |
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S8764New |
IITZ-01IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function. |
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S9424New |
Liensinine diperchlorateLiensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor. |
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S9150New |
DaurisolineDaurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects. |
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S1105 |
LY294002LY294002 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. |
![]() ![]() 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). |
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S1150 |
PaclitaxelPaclitaxel is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells. |
![]() ![]() (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.
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S2758 |
WortmanninWortmannin 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. |
![]() ![]() 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. |
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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. Solutions of 3-MA are best fresh-prepared by heating. |
![]() ![]() 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.
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S2775 |
NocodazoleNocodazole 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. |
![]() ![]() 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. |
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S4157 |
Chloroquine PhosphateChloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. |
![]() ![]() 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. |
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S1835 |
AzithromycinAzithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections. |
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S7289 |
PFK15PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. |
![]() ![]() 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
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S7885 |
SBI-0206965SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. |
![]() ![]() 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. |
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S8576 |
EAD1EAD1 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. |
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S7888 |
Spautin-1Spautin-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. |
![]() ![]() 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.
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S8317 |
3BDO3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. |
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S7811 |
MHY1485MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy. |
![]() ![]() MYH1485, an activator of mTOR, reduced LC3II production and inhibited autophagosome formation in PAR2-knockdown cells.
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S8596 |
AutophinibAutophinib 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. |
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S3758 |
Sinomenine hydrochlorideSinomenine (SN), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent. |
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S8369 |
Lys05Lys05 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. |
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S4430 |
Hydroxychloroquine SulfateHydroxychloroquine 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. |
![]() ![]() 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).
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S7949 |
MRT68921 HClMRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. |
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S7683 |
PIK-IIIPIK-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. |
![]() ![]() 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 |
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S8527 |
ROC-325ROC-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. |
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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. |
![]() ![]() 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. |
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S1002 |
ABT-737ABT-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. |
![]() ![]() 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. |
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S1049 |
Y-27632 2HClY-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. |
![]() ![]() 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.
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S1039 |
Rapamycin (Sirolimus)Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells. |
![]() ![]() 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). |
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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. |
![]() ![]() 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. |
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S9027New |
CorynoxineCorynoxine, a natural oxindole alkaloid, is a new autophagy enhancer. |
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S9310New |
IsorhychophyllineIsorhynchophylline 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. |
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S5312New |
Urolithin AUrolithin A, a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption. |
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S8595New |
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. |
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S1057 |
Obatoclax Mesylate (GX15-070)Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3. |
![]() ![]() 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.
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S1038 |
PI-103PI-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. |
![]() ![]() (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.
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S1149 |
Gemcitabine HClGemcitabine 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. |
![]() ![]() 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. |
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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. |
![]() ![]() 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).
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S1237 |
TemozolomideTemozolomide 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. |
![]() ![]() 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).
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S1950 |
Metformin HClMetformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). |
![]() ![]() 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.
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S1573 |
Fasudil (HA-1077) HClFasudil(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. |
![]() ![]() 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. |
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S1972 |
Tamoxifen CitrateTamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. |
![]() ![]() 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. |
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S2827 |
Torin 1Torin 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. |
![]() ![]() 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.
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S1396 |
ResveratrolResveratrol 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. |
![]() ![]() 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.
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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. |
![]() ![]() 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. |
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S1714 |
GemcitabineGemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. |
![]() ![]() 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. |
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S7046 |
Brefeldin ABrefeldin 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. |
![]() ![]() Immunofluorescence staining of LC3 protein expression of U2OS cells treated with DMSO (negative control), Rap (positive control, 500 nM), Tha (1 μM), Tun (2 μg/mL), BFA (10 μg/mL), and DTT (4 mM) for 8 h. Immunoblot of ER-phagy-related proteins of U2OS cells treated with four ER stress inducers.
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S2713 |
GeldanamycinGeldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. |
![]() ![]() 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.
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S2929 |
Pifithrin-α (PFTα) HBrPifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. |
![]() ![]() (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.
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S3030 |
NiclosamideNiclosamide 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). |
![]() ![]() 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.
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S1389 |
OmeprazoleOmeprazole is a proton pump inhibitor, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome. |
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S1979 |
Amiodarone HClAmiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias. |
![]() ![]() 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.
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S2480 |
Loperamide HClLoperamide HCl is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
![]() ![]() 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. |
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S4028 |
Dexamethasone Sodium PhosphateDexamethasone 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. |
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S1693 |
CarbamazepineCarbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes. |
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S2458 |
Clonidine HClClonidine HCl is a direct-acting α2 adrenergic agonist with an ED50 of 0.02±0.01 mg/kg. |
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S1837 |
FlubendazoleFlubendazole 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.
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S1747 |
NimodipineNimodipine is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure. |
![]() ![]() 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. |
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S3124 |
Dexamethasone AcetateDexamethasone 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. |
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S2491 |
NitrendipineNitrendipine is a dihydropyridine calcium channel blocker with an IC50 of 95 nM. |
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S3653 |
Spermidine trihydrochlorideSpermidine, 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). |
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S4081 |
Sulfacetamide SodiumSulfacetamide Sodium is an anti-biotic. |
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S8240 |
SMER28SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells. |
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S1238 |
TamoxifenTamoxifen is an antagonist of the estrogen receptor in breast tissue. |
![]() ![]() 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. |
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S1241 |
Vincristine sulfateVincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. |
![]() ![]() 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.
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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. |
![]() ![]() (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.
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S1041 |
STF-62247STF-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+). |
![]() ![]() 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. |
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S4750 |
Sulfacetamide sodium salt hydrateSulfacetamide 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. |