Autophagy

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S7683New

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.

S7949New

MRT68921

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.

S1105

LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

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.

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.

S4157

Chloroquine Phosphate

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

S1389

Omeprazole

Omeprazole is a proton pump inhibitor, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.

S1835

Azithromycin

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

S7885

SBI-0206965

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

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.

S7811

MHY1485

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

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.

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.

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.

S8240New

SMER28

SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.

S1208

Doxorubicin (Adriamycin)

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

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.

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) HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM 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 is a phytoalexin produced naturally by several plants with 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 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.

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)

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

S3030

Niclosamide

Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of 0.7 μM in a cell-free assay.

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.

S4081

Sulfacetamide Sodium

Sulfacetamide Sodium is an anti-biotic.

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue.

Catalog No. Information Product Use Citations Product Validations
S7683New

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.

S7949New

MRT68921

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.

S1105

LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

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.

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.

S4157

Chloroquine Phosphate

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

S1389

Omeprazole

Omeprazole is a proton pump inhibitor, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.

S1835

Azithromycin

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

S7885

SBI-0206965

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

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.

S7811

MHY1485

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

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.

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.

2015, 10.1038/nbt.3130

2011, 29(3):255-65

2011, 471(7337):235-9

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.

2011, 29(6):542-6

2013, 19(11):1478-88

2012, 46(5):573-83

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.

2016, 532(7597):107-11

2013, 23(10):1187-200

2015, 10.1182/blood-2014-07-590646

S1039

Rapamycin (Sirolimus)

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

2016, 539(7629):437-442

2014, 46(4):364-70

2011, 19(6):792-804

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.

2012, 151(5):937-50

2012, 44(8):852-60

2015, 27(4):533-46

S8240New

SMER28

SMER28 is a small-molecule enhancer (SMER) of autophagy, inducing autophagy independently of rapamycin in mammalian cells.

S1208

Doxorubicin (Adriamycin)

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

2015, 7(284):284ra57

2014, 5:3384

2015, 112(6):1839-44

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.

2015, 10.1038/nchembio.1986

2012, 72(12):3069-79

2011, 71(13):4494-505

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.

2013, 153(4):840-54

2013, 27(3):650-60

2012, 26(5):927-33

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.

2015, 7(284):284ra57

2014, 42(10):6436-47

2014, 20(12):3187-97

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.

2016, 353(6302):929-32

2015, 10.1172/JCI78018

2013, 9(11):708-14

S1950

Metformin HCl

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

2014, 26(6):840-50

2015, 6(2):969-78

2016, 6:28611

S1573

Fasudil (HA-1077) HCl

Fasudil (HA-1077) HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively.

2014, 124(9):3757-66

2014, 124(4):1646-59

2013, 62(5):1697-708

S1972

Tamoxifen Citrate

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

2014, Timothy E. Richardson

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.

2016, 6(7):727-39

2015, 4

2014, 34(24):4474-84

S1396

Resveratrol

Resveratrol is a phytoalexin produced naturally by several plants with anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.

2016,

2016, 1859(2):294-305

2015, 35(6):2255-2271

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.

2013, 32(10):1316-29

2016, 46(10):948-52

S1714

Gemcitabine

Gemcitabine is a very potent and specific deoxycytidine analogue, used as chemotherapy.

2015, 7(284):284ra57

2015, 112(6):1839-44

2014, 42(10):6436-47

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.

2016, 6:25118

2014, 289(32):22284-305

2014, 156(2):141-153

S2713

Geldanamycin

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

2015, 10.1093/jac/dku549

2014, 5(12):4269-82

2015, 59(8):4727-33

S2929

Pifithrin-α (PFTα)

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

2015, 15(12):3095-111

2014, 88(2):385-94

2015, 20(6):787-95

S3030

Niclosamide

Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of 0.7 μM in a cell-free assay.

2016, 36:199-204

S1979

Amiodarone HCl

Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.

2015, 285(1):51-60

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.

2014, 58(8):4875-84

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.

2016, 132:38-45

2016, 132:38-45

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.

S4081

Sulfacetamide Sodium

Sulfacetamide Sodium is an anti-biotic.

S1238

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue.

2015, 6(4):2315-30

2014, Timothy E. Richardson

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.

2013, 73(20):6310-22

2014, 350(3):646-56

2012, 13(9):10736-49

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.

2015, 10.1038/nbt.3130

2013, 33(17):7535-47

2016, 7:e2221