Mitophagy

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cell Rep, 2022, 38(11):110522
Oncogene, 2022, 10.1038/s41388-022-02197-x
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), 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.
Autophagy, 2022, 1-19
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA, NSC 66389) 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.
Nature, 2022, 603(7899):159-165
Autophagy, 2022, 10.1080/15548627.2022.2055285
Nat Commun, 2022, 13(1):846
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.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
PLoS One, 2022, 17(3):e0265805
Nat Cell Biol, 2021, 10.1038/s41556-021-00704-y
S7162 Mdivi-1 Mdivi-1 (Mitochondrial division inhibitor 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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
Oxid Med Cell Longev, 2022, 2022:3745135
Cancer Discov, 2022, 12(1):250-269
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.
S0881 Mitochonic acid 5 Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Neural Regen Res, 2021, 16(9):1813-1820
Neural Regen Res, 2021, 16(9):1813-1820
Cell Mol Biol Lett, 2018, 23:14
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.
Signal Transduct Target Ther, 2022, 7(1):51
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) 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.
Clin Cancer Res, 2022, clincanres.4291.2021
Cancers (Basel), 2022, 14(4)903
Biomedicines, 2022, 10(2)321
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.
Cell, 2022, 185(1):169-183.e19
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 24(1):51-61
S1076 Adezmapimod (SB203580) Adezmapimod (SB203580, RWJ 64809, PB 203580) 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.
Cancer Cell, 2022, 40(2):168-184.e13
Bone Res, 2022, 10(1):27
J Immunother Cancer, 2022, 10(3)e004414
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 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 3.
Blood Cancer J, 2022, 12(3):39
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Cell Mol Med, 2022, 10.1111/jcmm.17210
S1168 Valproic Acid (NSC 93819) sodium salt Valproic Acid sodium salt (NSC 93819, 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. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13014
Front Immunol, 2021, 12:771453
Front Oncol, 2021, 11:723966
S1204 Melatonin (NSC 113928) Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) 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.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
Int J Mol Sci, 2021, 22(11)5649
Int Immunopharmacol, 2021, 96:107787
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) 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.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
EMBO Mol Med, 2022, 14(2):e14903
EMBO J, 2022, 10.15252/embj.2021108599
S1225 Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.
Mol Cell, 2022, S1097-2765(22)00085-5
Dev Cell, 2022, 57(5):638-653.e5
Cancers (Basel), 2022, 14(6)1537
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) 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.
Mol Oncol, 2021, 10.1002/1878-0261.12936
Aging (Albany NY), 2021, 13(12):16816-16833
Molecules, 2021, 26(14)4124
S1322 Dexamethasone (MK-125) Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) 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.
Hepatology, 2022, 10.1002/hep.32436
Nat Commun, 2022, 13(1):1009
J Immunother Cancer, 2022, 10(1)e003766
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
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.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
Sci Immunol, 2022, 7(68):eabf2846
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-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.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1792 Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) 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.
PLoS Pathog, 2022, 18(4):e1010468
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Theranostics, 2021, 11(4):1609-1625
S1802 AICAR (Acadesine) AICAR (Acadesine, NSC105823, AICA Riboside), 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.
Signal Transduct Target Ther, 2022, 7(1):66
Food Funct, 2022, 10.1039/d1fo03752h
Cell Res, 2021, 10.1038/s41422-021-00565-y
S1950 Metformin HCl Metformin HCl (1,1-Dimethylbiguanide 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.
Cell Death Discov, 2022, 8(1):204
Int Immunopharmacol, 2022, 108:108683
Bioengineered, 2022, 13(2):3911-3929
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. Torkinib (PP242) induces mitophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Nat Commun, 2022, 13(1):1548
Life Sci Alliance, 2022, 5(6)e202101169
S2348 Rotenone (Barbasco) Rotenone (Barbasco, Dactinol, Paraderil, Rotenon, Rotocide) 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.
Sci Signal, 2022, 15(721):eabi9983
Food Funct, 2022, 10.1039/d1fo03909a
Nature, 2021, 10.1038/s41586-021-04049-2
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
Nucleic Acids Res, 2021, gkab538
S2730 Crenolanib (CP-868596) Crenolanib (CP-868596, ARO 002) 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.
Mol Cancer Ther, 2022, OF1-OF11
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
S3017 Aspirin (NSC 27223) Aspirin (NSC 27223, Acetylsalicylic acid, ASA) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Dev Cell, 2021, S1534-5807(21)00485-8
Pigment Cell Melanoma Res, 2021, 10.1111/pcmr.13021
S3944 Valproic acid (VPA) Valproic acid (VPA, 2-Propylvaleric Acid, Valproate) is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase (HDAC) inhibitor and is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Valproic acid activates Notch-1 signaling.
Front Immunol, 2021, 12:771453
Sci China Life Sci, 2021, 10.1007/s11427-020-1855-4
Anticancer Res, 2021, 41(2):687-697
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Blood, 2022, blood.2021012366
S5312 Urolithin A Urolithin A (3,8-Dihydroxy Urolithin, 2',7-Dihydroxy-3,4-benzocoumarin), a metabolite of ellagitannin, is a first-in-class natural compound that induces mitophagy both in vitro and in vivo following oral consumption.
Neuropharmacology, 2022, 207:108963
Neural Regen Res, 2022, 17(9):2007-2013
Food Funct, 2022, 13(1):375-385
S5958 Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Cell Death Discov, 2022, 8(1):204
Int Immunopharmacol, 2022, 108:108683
Cell Res, 2021, 10.1038/s41422-021-00565-y
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties. Salidroside is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
FASEB J, 2021, 35(12):e22044
Curr Med Sci, 2021, 10.1007/s11596-021-2374-6
J Med Virol, 2019, 91(8):1440-1447
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.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cell Rep, 2022, 38(11):110522
Oncogene, 2022, 10.1038/s41388-022-02197-x
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), 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.
Autophagy, 2022, 1-19
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA, NSC 66389) 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.
Nature, 2022, 603(7899):159-165
Autophagy, 2022, 10.1080/15548627.2022.2055285
Nat Commun, 2022, 13(1):846
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.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
PLoS One, 2022, 17(3):e0265805
Nat Cell Biol, 2021, 10.1038/s41556-021-00704-y
S7162 Mdivi-1 Mdivi-1 (Mitochondrial division inhibitor 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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
Oxid Med Cell Longev, 2022, 2022:3745135
Cancer Discov, 2022, 12(1):250-269
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.
S0881 Mitochonic acid 5 Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis.
Neural Regen Res, 2021, 16(9):1813-1820
Neural Regen Res, 2021, 16(9):1813-1820
Cell Mol Biol Lett, 2018, 23:14
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.
Signal Transduct Target Ther, 2022, 7(1):51
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) 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.
Clin Cancer Res, 2022, clincanres.4291.2021
Cancers (Basel), 2022, 14(4)903
Biomedicines, 2022, 10(2)321
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.
Cell, 2022, 185(1):169-183.e19
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Cell Biol, 2022, 24(1):51-61