Mitophagy

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1102 U0126-EtOH <1 mg/mL 85 mg/mL ''<1 mg/mL
S2767 3-Methyladenine (3-MA) 10 mg/mL 3 mg/mL '4 mg/mL
S7046 Brefeldin A <1 mg/mL 4 mg/mL '<1 mg/mL
S1759 Pitavastatin Calcium <1 mg/mL 51 mg/mL ''<1 mg/mL
S7162 Mdivi-1 <1 mg/mL 70 mg/mL '<1 mg/mL
S9424 Liensinine diperchlorate -1 mg/mL 50 mg/mL -1 mg/mL
S1060 Olaparib (AZD2281) 0.002 mg/mL 86 mg/mL <1 mg/mL
S1002 ABT-737 <1 mg/mL 100 mg/mL '<1 mg/mL
S1378 Ruxolitinib (INCB018424) <1 mg/mL 61 mg/mL 61 mg/mL
S1042 Sunitinib Malate <1 mg/mL 15 mg/mL ''<1 mg/mL
S1076 SB203580 <1 mg/mL 43 mg/mL '<1 mg/mL
S1208 Doxorubicin (Adriamycin) HCl 20 mg/mL 100 mg/mL <1 mg/mL
S1141 Tanespimycin (17-AAG) <1 mg/mL 100 mg/mL '5 mg/mL
S1225 Etoposide <1 mg/mL 100 mg/mL '''<1 mg/mL
S2730 Crenolanib (CP-868596) <1 mg/mL 88 mg/mL '7 mg/mL
S1950 Metformin HCl 33 mg/mL <1 mg/mL '<1 mg/mL
S1802 AICAR (Acadesine) <1 mg/mL 51 mg/mL '<1 mg/mL
S1396 Resveratrol <1 mg/mL 45 mg/mL ''<1 mg/mL
S1322 Dexamethasone <1 mg/mL 79 mg/mL '''6 mg/mL
S1792 Simvastatin <1 mg/mL 83 mg/mL '83 mg/mL
S1290 Celastrol <1 mg/mL 90 mg/mL ''<1 mg/mL
S1204 Melatonin <1 mg/mL 47 mg/mL '47 mg/mL
S3017 Aspirin <1 mg/mL 36 mg/mL '36 mg/mL
S5312 Urolithin A <1 mg/mL 45 mg/mL <1 mg/mL
S5243 Ruxolitinib Phosphate 29 mg/mL 80 mg/mL '8 mg/mL
S2348 Rotenone (Barbasco) <1 mg/mL 55 mg/mL 2 mg/mL
S2396 Salidroside 60 mg/mL 60 mg/mL 4 mg/mL

Mitophagy製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1102

U0126-EtOH

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

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. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.

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. Brefeldin A is also an inhibitor of autophagy and mitophagy.

S1759

Pitavastatin Calcium

Pitavastatin Calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.

S7162

Mdivi-1

Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 μM. Mdivi-1 attenuates mitophagy and enhances apoptosis.

S9424

Liensinine diperchlorate

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

S1060

Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

S1378

Ruxolitinib (INCB018424)

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

S1042

Sunitinib Malate

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

S1076

SB203580

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

S1141

Tanespimycin (17-AAG)

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 2.

S1225

Etoposide

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.

S2730

Crenolanib (CP-868596)

Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy.

S1950

Metformin HCl

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.

S1802

AICAR (Acadesine)

AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.

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. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

S1322

Dexamethasone

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

S1792

Simvastatin

Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.

S1290

Celastrol

Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.

S1204

Melatonin

Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.

S3017

Aspirin

Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.

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.

S5243

Ruxolitinib Phosphate

Ruxolitinib Phosphate is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

S2348

Rotenone (Barbasco)

Rotenone is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

S2396

Salidroside

Salidroside, a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1102

U0126-EtOH

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

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. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.

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. Brefeldin A is also an inhibitor of autophagy and mitophagy.

S1759

Pitavastatin Calcium

Pitavastatin Calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.

S7162

Mdivi-1

Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 μM. Mdivi-1 attenuates mitophagy and enhances apoptosis.

S9424

Liensinine diperchlorate

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

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1060

Olaparib (AZD2281)

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations.

2020, 15 pii: S1535-6108(20)30164-1

2020, 37(2):157-167

2020, 37(3):340-353

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. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.

2020, 14(3):3378-3388

2020, 11(1):259

2020, 10.1158/0008-5472.CAN-19-1784

S1378

Ruxolitinib (INCB018424)

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

2020, 13;37(1):104-122e12

2020, 12;blood.2020006075

2020, 11;27(3):476-485 e7

S1042

Sunitinib Malate

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

2020, 15(2):421-449

2020, 9(3)

2020, 19;20:58

S1076

SB203580

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

2020, 4;31(2):406-421 e7

2020, 11(1):37

2020, 8;11(1):2286

S1208

Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

2020, 24;11(1):1972

2020, 23;18(3):e3000666

2020, 10.1158/0008-5472.CAN-19-2069

S1141

Tanespimycin (17-AAG)

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 2.

2020, 29;11(1):2086

2020, 7;12(4)

2020, 4;10(5):1585-1597

S1225

Etoposide

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.

2020, 22 pii: S1097-2765(20)30231-8

2020, 6

2020, 1;34(9-10):637-649

S2730

Crenolanib (CP-868596)

Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. Crenolanib helps to induce mitophagy.

2020, 7;26(5):707-721e5

2020, 23;canres37312019

2020, 10:102444

S1950

Metformin HCl

Metformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.

2020, 11(1):3344

2020, 8;11(6):427

2020, 56(5):1140-1151

S1802

AICAR (Acadesine)

AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.

2020, 8;11(6):427

2020, 22(2):e13131

2020, 20;10:43

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. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

2020, 133:115252

2020, 13;295(11):3485-3496

2020, 19(4):3269-3277

S1322

Dexamethasone

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

2020, 10(6):72

2020, 16(4):543-552

2020, 1-10

S1792

Simvastatin

Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.

2020, 44187

2020, 6;8(1):72

2020, 10(1):931

S1290

Celastrol

Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.

2018, 315(4):F954-F966

2017, 136:63-73

2016, 12(10):e1005929

S1204

Melatonin

Melatonin is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.

2020, 27(1):75-86

2019, 9(13):3768-3779

2019, 25:101197

S3017

Aspirin

Aspirin is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.

2020, 52(2):328-341

2020, 16;16(3):e1008341

2020, 14(2):162-180

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.

S5243

Ruxolitinib Phosphate

Ruxolitinib Phosphate is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

2020, 12;blood.2020006075

2020, 117(26):15047-15054

2020, 29;201918307

S2348

Rotenone (Barbasco)

Rotenone is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.

2020, 4;10(5):1585-1597

2019, 10(1):3856

2018, 55(5):4078-4089

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2396

Salidroside

Salidroside, a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.