| S5312 |
Urolithin A
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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.
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Int J Mol Sci, 2024, 25(15)8246
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Cell Commun Signal, 2023, 21(1):357
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Biomedicines, 2023, 11(4), 1125
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| S0881 |
Mitochonic acid 5 (MA-5)
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Mitochonic acid 5 (MA-5) reduces mitochondrial apoptosis via upregulation of mitophagy, regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway, and modulates mitochondrial ATP synthesis.
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Front Cell Dev Biol, 2025, 13:1583951
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Animals (Basel), 2024, 14(3):368.
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Animals (Basel), 2024, 14(3)368
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| E2988 |
Sulfosuccinimidyl Oleate Sodium (SSO)
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Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain with IC50 of 4 μM. It inhibits CD36 mediated LCFA transport. It exhibits anti-inflammatory effect.
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Int J Biol Sci, 2025, 21(5):2118-2134
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Sci Rep, 2025, 15(1):30552
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Front Cell Dev Biol, 2021, 9:687169
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| E1462 |
P62-mediated mitophagy inducer
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P62-mediated mitophagy inducer (PMI) is a P62-mediated activator of mitophagy that functions independently of parkin recruitment or mitochondrial membrane potential (ΔΨm) collapse. It remains effective even in cells lacking a fully functional PINK1/Parkin pathway. PMI stabilizes Nrf2 and enhances p62 expression, thereby activating mitophagy.
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| S1076 |
SB203580 (Adezmapimod)
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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.
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Cell Res, 2025, 10.1038/s41422-025-01085-9
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Cell Mol Immunol, 2025, 22(5):541-556
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Nat Cancer, 2025, 6(2):259-277
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| S1102 |
U0126-EtOH
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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.
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Nat Commun, 2025, 16(1):2192
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Nat Commun, 2025, 16(1):7156
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Adv Sci (Weinh), 2025, 12(44):e11726
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| S1002 |
ABT-737
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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.
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Signal Transduct Target Ther, 2025, 10(1):161
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J Hepatol, 2025, S0168-8278(24)02830-7
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Cell Rep Med, 2025, S2666-3791(25)00057-6
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| S1042 |
Sunitinib (SU11248) Malate
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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.
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Nat Commun, 2025, 16(1):7853
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CNS Neurosci Ther, 2025, 31(12):e70696
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Sci Rep, 2025, 15(1):35889
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| S1802 |
AICAR (Acadesine)
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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. This compound induces mitophagy. Phase 3.
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Nat Commun, 2025, 16(1):8478
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Theranostics, 2025, 15(15):7567-7583
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Glia, 2025, 73(11):2253-2272
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| S1141 |
Tanespimycin (17-AAG)
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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.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Autophagy, 2025, 1-23.
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Cell Commun Signal, 2025, 23(1):331
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| S2218 |
Torkinib (PP242)
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Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; this compound targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. It induces mitophagy and apoptosis.
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J Immunother Cancer, 2025, 13(3)e010753
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Cell Rep, 2025, 44(4):115452
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Int J Mol Sci, 2025, 26(16)7770
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| S7162 |
Mdivi-1
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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.
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J Hazard Mater, 2025, 495:138854
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Redox Biol, 2025, 86:103818
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J Nanobiotechnology, 2025, 23(1):437
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| S2730 |
Crenolanib (CP-868596)
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Crenolanib 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.
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Cancer Cell, 2025, S1535-6108(25)00070-4
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Nat Commun, 2025, 16(1):1358
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J Extracell Vesicles, 2025, 14(9):e70163
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| S7046 |
Brefeldin A (BFA chemical)
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Brefeldin A (BFA) 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.
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Protein Cell, 2025, pwaf020
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Cancer Commun (Lond), 2025, 10.1002/cac2.70036
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J Integr Plant Biol, 2025, 67(8):2229-2244
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| S1396 |
Resveratrol (trans-Resveratrol)
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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.
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Aging Cell, 2025, e70075
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Biomed Pharmacother, 2025, 190:118393
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Breast Cancer Res, 2025, 27(1):186
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| S5958 |
Metformin (1,1-Dimethylbiguanide)
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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.
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Signal Transduct Target Ther, 2025, 10(1):271
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Theranostics, 2025, 15(17):9029-9046
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Int J Biol Sci, 2025, 21(9):4231-4251
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| S3944 |
VPA (Valproic acid)
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Valproic acid (VPA) 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. This compound induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α. Additionally, it activates Notch-1 signaling.
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Cell, 2025, S0092-8674(25)00406-4
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Nat Commun, 2025, 16(1):8267
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Stem Cell Res Ther, 2025, 16(1):426
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| S1168 |
Valproic Acid sodium
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Valproic Acid sodium 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.
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J Exp Clin Cancer Res, 2024, 43(1):152
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J Immunother Cancer, 2024, 12(11)e009805
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Front Pharmacol, 2024, 15:1534772
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| S1204 |
Melatonin
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Melatonin is a MT receptor agonist, used as a dietary supplement. This compound is a selective ATF-6 inhibitor and downregulates COX-2. It enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
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Antioxidants (Basel), 2025, 14(5)528
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Sci Rep, 2025, 15(1):8451
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Biochem Biophys Res Commun, 2025, 760:151706
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| S1290 |
Celastrol
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Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. This compound induces apoptosis and autophagy via the ROS/JNK signaling pathway. It inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
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World J Gastroenterol, 2025, 31(23):106949
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Adipocyte, 2025, 14(1):2548787
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MedComm (2020), 2024, 5(12):e70033
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| S3017 |
Aspirin
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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. This compound induces autophagy and stimulates mitophagy.
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J Biol Chem, 2025, 301(2):108195
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PLoS One, 2025, 20(9):e0332825
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iScience, 2024, 27(10):110862
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| S1351 |
Ivermectin
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Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. This compound is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). It is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. This chemical induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
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Nat Commun, 2025, 16(1):7156
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J Adv Res, 2025, S2090-1232(25)00874-4
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Biomed Pharmacother, 2025, 189:118248
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| S2396 |
Salidroside
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Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties. This compound is a prolyl endopeptidase inhibitor. It alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. This chemical protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
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PLoS One, 2024, 19(7):e0306926
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Mol Med Rep, 2023, 27(2)37
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Research Square, 2023, 10.21203/rs.3.rs-3696850/v1
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| S9424 |
Liensinine diperchlorate
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Liensinine, 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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