Autophagy

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Autophagy Products

New Autophagy Products
Catalog No. Information Product Use Citations Product Validations
S6471New

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.

S8793New

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.

S8807New

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.

S8808New

DC661

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

S8744New

PHY34

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

S5920New

CA-5f

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

S8764New

IITZ-01

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

S9424New

Liensinine diperchlorate

Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.

S9150New

Daurisoline

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

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.

S1150

Paclitaxel

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

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.

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.

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.

S4157

Chloroquine diphosphate

Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

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.

S7885

SBI-0206965

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

S8576

EAD1

EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.

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.

S8317

3BDO

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

S7811

MHY1485

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

S8596

Autophinib

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.

S3758

Sinomenine 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.

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.

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.

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.

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.

S1049

Y-27632 2HCl

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

S1039

Rapamycin (Sirolimus)

Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

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.

S9027New

Corynoxine

Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.

S9310New

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.

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.

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.

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.

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.

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.

S1950

Metformin HCl

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

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.

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.

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.

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.

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.

S1714

Gemcitabine

Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy.

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.

S2713

Geldanamycin

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

S2929

Pifithrin-α (PFTα) HBr

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

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).

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.

S2480

Loperamide HCl

Loperamide 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.

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.

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.

S1747

Nimodipine

Nimodipine is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.

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.

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.

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.

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.

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.

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.

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+).

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.

Catalog No. Information Product Use Citations Product Validations
S6471New

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.

S8793New

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.

S8807New

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.

S8808New

DC661

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

S8744New

PHY34

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

S5920New

CA-5f

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

S8764New

IITZ-01

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

S9424New

Liensinine diperchlorate

Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.

S9150New

Daurisoline

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

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.

S1150

Paclitaxel

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

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.

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.

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.

S4157

Chloroquine diphosphate

Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

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.

S7885

SBI-0206965

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

S8576

EAD1

EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.

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.

S8317

3BDO

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

S7811

MHY1485

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

S8596

Autophinib

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.

S3758

Sinomenine 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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S1047

Vorinostat (SAHA, MK0683)

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

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.

S1049

Y-27632 2HCl

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

S1039

Rapamycin (Sirolimus)

Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

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.

S9027New

Corynoxine

Corynoxine, a natural oxindole alkaloid, is a new autophagy enhancer.

S9310New

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.

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.

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.

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.

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.

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.

S1950

Metformin HCl

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis).

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.

S1972

Tamoxifen Citrate

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.

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.

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.

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.

S1714

Gemcitabine

Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy.

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.

S2713

Geldanamycin

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

S2929

Pifithrin-α (PFTα) HBr

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

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).

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.

S2480

Loperamide HCl

Loperamide 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.

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.

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.

S1747

Nimodipine

Nimodipine is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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+).

Catalog No. Information Product Use Citations Product Validations
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.