Mitophagy

Mitophagy製品

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  • Mitophagy阻害剤 (6)
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S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
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 ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。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.
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 ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
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 (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.
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.
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
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
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.
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
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
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.
S1060 Olaparib (AZD2281) オラパリブ (Olaparib (AZD2281, KU0059436)) は選択的 PARP1/2 阻害剤であり、cell-free assay における IC50 はそれぞれ 5 nM および 1 nM です。タンキラーゼ-1 (Tankyrase-1) に対しては 1/300 の効果を示します。オラパリブは BRCA に変異をきたした細胞において、マイトファジー (mitophagy) に関連した顕著なオートファジー (mitophagy) を誘発します。
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 ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の 基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。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.
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 ルクソリチニブ (Ruxolitinib (INCB018424)) は、最初に臨床試験が行われた強力で選択的なJAK1/2 阻害剤であり、IC50 はそれぞれ 3.3 nM/ 2.8 nM、JAK1/2 に対して JAK3 の 130 倍の選択性を示します。ルクソリチニブはマイトファジー (mitophagy) によって抗腫瘍作用を示します。また、オートファジー (autophagy) を誘導し、アポトーシス (apoptosis) を促進します。
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 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 (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.
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
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
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
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
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.
PLoS One, 2024, 19(7):e0306926
Mol Med Rep, 2023, 27(2)37
Research Square, 2023, 10.21203/rs.3.rs-3696850/v1

Mitophagy阻害剤の選択性比較

Tags: Mitophagy inhibitor|Mitophagy agonist|Mitophagy activator|Mitophagy inducer|Mitophagy antagonist|Mitophagy signaling pathway|Mitophagy assay kit