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. |
-
Nature, 2024, 10.1038/s41586-024-07217-2
-
Nature, 2024, 628(8007):433-441
-
Cell, 2024, 187(4):945-961.e18
|
|
S1208 |
Doxorubicin (DOX) HCl
|
Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase I and topoisomerase II with IC50s of 0.8 μM and 2.67 μM, respectively. 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.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.Doxorubicin (Adriamycin) HCl can be used to induce animal models of kidney disease.
|
-
Cell Metab, 2024, S1550-4131(24)00371-1
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nucleic Acids Res, 2024, gkae811
|
|
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. |
-
Nat Commun, 2024, 15(1):987
-
Nat Commun, 2024, 15(1):1300
-
Acta Pharm Sin B, 2024, 14(4):1693-1710
|
|
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. |
-
MedComm (2020), 2024, 5(5):e525
-
Int J Biol Sci, 2024, 20(6):2202-2218
-
Cell Death Dis, 2024, 15(1):31
|
|
S1378 |
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. |
-
Nat Commun, 2024, 15(1):2503
-
Nat Commun, 2024, 15(1):8663
-
Nat Commun, 2024, 15(1):2989
|
|
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. |
-
Gastroenterology, 2024, S0016-5085(24)00062-3
-
Nat Commun, 2024, 15(1):830
-
Nat Commun, 2024, 15(1):1041
|
|
S1225 |
Etoposide
|
Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis. |
-
Nature, 2024, 635(8037):201-209
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nat Commun, 2024, 15(1):9181
|
|
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. |
-
Virol J, 2024, 21(1):23
-
Int J Mol Sci, 2023, 24(7)6228
-
Front Oncol, 2023, 13:1043694
|
|
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. |
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
-
Pharmaceuticals (Basel), 2024, 17(1)108
-
Cell Cycle, 2024, 1-13.
|
|
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. |
-
J Clin Invest, 2024, 134(22)e181314
-
J Clin Invest, 2024, e175023
-
Research (Wash D C), 2024, 7:0400
|
|
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. |
-
Cell, 2024, S0092-8674(24)00583-X
-
Cell, 2024, S0092-8674(24)00583-X
-
Theranostics, 2024, 14(6):2442-2463
|
|
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. |
-
Mol Cell, 2024, S1097-2765(24)00832-3
-
Cell Death Dis, 2024, 15(1):48
-
Mol Oncol, 2024, 10.1002/1878-0261.13716
|
|
S2730 |
Crenolanib
|
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. |
-
Signal Transduct Target Ther, 2024, 9(1):193.
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
-
Cell Death Discov, 2023, 9(1):44
|
|
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. |
-
Cell Host Microbe, 2024, S1931-3128(24)00005-2
-
Nat Commun, 2024, 15(1):7991
-
Nat Commun, 2024, 15(1):1176
|
|
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. |
-
Nat Commun, 2024, 15(1):1785
-
J Clin Invest, 2024, e175023
-
EBioMedicine, 2024, 102:105090
|
|
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. |
-
Immunity, 2024, 57(2):287-302.e12
-
Nat Commun, 2024, 15(1):1669
-
Autophagy, 2024, 1-22.
|
|
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. |
-
Biochem Biophys Res Commun, 2024, 723:150186
-
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
-
Cell Death Dis, 2023, 14(6):367
|
|
S7046 |
Brefeldin A (BFA)
|
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. |
-
Nat Commun, 2024, 15(1):203
-
Cancer Commun (Lond), 2024, 10.1002/cac2.12583
-
Cell Rep Med, 2024, S2666-3791(24)00544-5
|
|
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. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cancer Med, 2024, 13(12):e7393
-
Neuron, 2023, S0896-6273(23)00513-5
|
|
S2391 |
Quercetin
|
Quercetin, 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. |
-
Cell Metab, 2024, S1550-4131(24)00371-1
-
Nucleic Acids Res, 2024, gkae322
-
Clin Transl Med, 2024, 14(5):e1660
|
|
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. |
-
J Clin Invest, 2024, 134(22)e181314
-
Adv Healthc Mater, 2024, e2303785.
-
Cell Rep, 2024, 43(10):114775
|
|
S1168 |
Valproic Acid sodium
|
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. |
-
J Exp Clin Cancer Res, 2024, 43(1):152
-
J Immunother Cancer, 2024, 12(11)e009805
-
Sci Total Environ, 2022, 838(Pt 2):155825
|
|
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. |
-
Heliyon, 2024, 10(18):e38098
-
Heliyon, 2024, 10(11):e32571
-
Zhejiang Da Xue Xue Bao Yi Xue Ban, 2024, 53(4):498-508
|
|
S3944 |
VPA (Valproic acid)
|
VPA (Valproic acid) 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. |
-
Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
-
Nat Commun, 2024, 15(1):668
-
Dev Cell, 2024, S1534-5807(24)00326-5
|
|
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. |
-
Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
-
iScience, 2023, 26(7):107105
-
Comput Struct Biotechnol J, 2022, 20:5750-5760
|
|
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. |
-
Int J Biol Sci, 2024, 20(14):5731-5746
-
Int J Mol Sci, 2024, 25(10)5237
-
Fundam Res, 2024, 4(2):394-400
|
|
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. |
-
Nat Commun, 2024, 15(1):4099
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cell Rep, 2024, 43(6):114286
|
|
S1351 |
Ivermectin
|
Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
-
J Clin Invest, 2024, 134(22)e181314
-
Viruses, 2024, 16(4)640
-
Life Sci Alliance, 2023, 6(8)e202302133
|
|
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. |
-
Int J Mol Sci, 2024, 25(15)8246
-
Cell Commun Signal, 2023, 21(1):357
-
Biomedicines, 2023, 11(4), 1125
|
|
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. |
-
PLoS One, 2024, 19(7):e0306926
-
Mol Med Rep, 2023, 27(2)37
-
Research Square, 2023, 10.21203/rs.3.rs-3696850/v1
|
|
S0881 |
Mitochonic acid 5 (MA-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. |
-
Animals (Basel), 2024, 14(3):368.
-
Animals (Basel), 2024, 14(3)368
-
J Ovarian Res, 2022, 15(1):103
|
|
E2988 |
Sulfosuccinimidyl oleate sodium
|
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. |
-
Front Cell Dev Biol, 2021, 9:687169
|
|
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. |
|
|
S2348 |
Rotenone
|
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. |
-
Cell Rep Med, 2024, 5(5):101519
-
Redox Biol, 2024, 70:103039
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
|
|
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. |
- Nature, 2024, 10.1038/s41586-024-07217-2
- Nature, 2024, 628(8007):433-441
- Cell, 2024, 187(4):945-961.e18
|
|
S1208 |
Doxorubicin (DOX) HCl
|
Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase I and topoisomerase II with IC50s of 0.8 μM and 2.67 μM, respectively. 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.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.Doxorubicin (Adriamycin) HCl can be used to induce animal models of kidney disease.
|
- Cell Metab, 2024, S1550-4131(24)00371-1
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nucleic Acids Res, 2024, gkae811
|
|
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. |
- Nat Commun, 2024, 15(1):987
- Nat Commun, 2024, 15(1):1300
- Acta Pharm Sin B, 2024, 14(4):1693-1710
|
|
S1378 |
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. |
- Nat Commun, 2024, 15(1):2503
- Nat Commun, 2024, 15(1):8663
- Nat Commun, 2024, 15(1):2989
|
|
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. |
- Gastroenterology, 2024, S0016-5085(24)00062-3
- Nat Commun, 2024, 15(1):830
- Nat Commun, 2024, 15(1):1041
|
|
S1225 |
Etoposide
|
Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis. |
- Nature, 2024, 635(8037):201-209
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nat Commun, 2024, 15(1):9181
|
|
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. |
- Virol J, 2024, 21(1):23
- Int J Mol Sci, 2023, 24(7)6228
- Front Oncol, 2023, 13:1043694
|
|
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. |
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
- Pharmaceuticals (Basel), 2024, 17(1)108
- Cell Cycle, 2024, 1-13.
|
|
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. |
- J Clin Invest, 2024, 134(22)e181314
- J Clin Invest, 2024, e175023
- Research (Wash D C), 2024, 7:0400
|
|
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. |
- Cell, 2024, S0092-8674(24)00583-X
- Cell, 2024, S0092-8674(24)00583-X
- Theranostics, 2024, 14(6):2442-2463
|
|
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. |
- Mol Cell, 2024, S1097-2765(24)00832-3
- Cell Death Dis, 2024, 15(1):48
- Mol Oncol, 2024, 10.1002/1878-0261.13716
|
|
S2730 |
Crenolanib
|
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. |
- Signal Transduct Target Ther, 2024, 9(1):193.
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
- Cell Death Discov, 2023, 9(1):44
|
|
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. |
- Cell Host Microbe, 2024, S1931-3128(24)00005-2
- Nat Commun, 2024, 15(1):7991
- Nat Commun, 2024, 15(1):1176
|
|
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. |
- Nat Commun, 2024, 15(1):1785
- J Clin Invest, 2024, e175023
- EBioMedicine, 2024, 102:105090
|
|
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. |
- Biochem Biophys Res Commun, 2024, 723:150186
- J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
- Cell Death Dis, 2023, 14(6):367
|
|
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. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cancer Med, 2024, 13(12):e7393
- Neuron, 2023, S0896-6273(23)00513-5
|
|
S2391 |
Quercetin
|
Quercetin, 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. |
- Cell Metab, 2024, S1550-4131(24)00371-1
- Nucleic Acids Res, 2024, gkae322
- Clin Transl Med, 2024, 14(5):e1660
|
|
S5958 |
Metformin
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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. |
- J Clin Invest, 2024, 134(22)e181314
- Adv Healthc Mater, 2024, e2303785.
- Cell Rep, 2024, 43(10):114775
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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. |
- J Exp Clin Cancer Res, 2024, 43(1):152
- J Immunother Cancer, 2024, 12(11)e009805
- Sci Total Environ, 2022, 838(Pt 2):155825
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S1204 |
Melatonin
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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. |
- Heliyon, 2024, 10(18):e38098
- Heliyon, 2024, 10(11):e32571
- Zhejiang Da Xue Xue Bao Yi Xue Ban, 2024, 53(4):498-508
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S3944 |
VPA (Valproic acid)
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VPA (Valproic acid) 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. |
- Sci Bull (Beijing), 2024, S2095-9273(24)00799-0
- Nat Commun, 2024, 15(1):668
- Dev Cell, 2024, S1534-5807(24)00326-5
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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. Aspirin induces autophagy and stimulates mitophagy. |
- Cell Death Discov, 2023, 10.1038/s41420-023-01664-y
- iScience, 2023, 26(7):107105
- Comput Struct Biotechnol J, 2022, 20:5750-5760
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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. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy. |
- Int J Biol Sci, 2024, 20(14):5731-5746
- Int J Mol Sci, 2024, 25(10)5237
- Fundam Res, 2024, 4(2):394-400
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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. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy. |
- J Clin Invest, 2024, 134(22)e181314
- Viruses, 2024, 16(4)640
- Life Sci Alliance, 2023, 6(8)e202302133
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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. |
- Int J Mol Sci, 2024, 25(15)8246
- Cell Commun Signal, 2023, 21(1):357
- 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. Mitochonic acid 5 regulates mitophagy via Bnip3 through the MAPK-ERK-Yap signaling pathway. Mitochonic acid 5 modulates mitochondrial ATP synthesis. |
- Animals (Basel), 2024, 14(3):368.
- Animals (Basel), 2024, 14(3)368
- J Ovarian Res, 2022, 15(1):103
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S2348 |
Rotenone
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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. |
- Cell Rep Med, 2024, 5(5):101519
- Redox Biol, 2024, 70:103039
- Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
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