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  • OXPHOS Inhibitors (11)
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Catalog No. Product Name Information Product Use Citations Product Validations
S8276 FCCP FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.
Autophagy, 2024, 1-22.
Theranostics, 2024, 14(4):1561-1582
iScience, 2024, 27(3):109265
S8731 IACS-010759 (IACS-10759) IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.
Nature, 2024, 10.1038/s41586-024-07812-3
Nat Commun, 2024, 15(1):8682
Nat Commun, 2024, 15(1):668
S8828 Gboxin Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.
Cell Rep, 2024, 43(10):114775
Mol Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S0096 S-Gboxin S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM.
Cell Rep Med, 2024, 5(10):101757
EMBO Mol Med, 2022, 14(12):e16082
S2987 4-Methyl-2-oxovaleric acid 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity.
E4709New MS-L6 MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy.
E1139 DX3-213B DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor with IC50 of 3.6 nM, and impairs ATP generation with IC50 of 11 nM.
S9604 Lixumistat (IM156) Lixumistat (IM156), is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
bioRxiv, 2024, 2024.09.16.613317
E1149 BAY-179 BAY-179 is an excellent in vivo suitable tool with which to probe the biological relevance of complex I inhibition in cancer indications.
S5604 Diphenylamine Hydrochloride Diphenylamine (N-Phenylbenzenamine, Anilinobenzene, C.I. 10355), a derivative of aniline, is widely used as an industrial antioxidant, dye mordant and reagent and is also employed in agriculture as a fungicide and antihelmintic. Diphenylamine can inhibits oxidative phosphorylationsignificantly, although its inhibition potency was weaker than that of NSAIDs with a diphenylamine structure.
S8276 FCCP FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.
Autophagy, 2024, 1-22.
Theranostics, 2024, 14(4):1561-1582
iScience, 2024, 27(3):109265
S8731 IACS-010759 (IACS-10759) IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.
Nature, 2024, 10.1038/s41586-024-07812-3
Nat Commun, 2024, 15(1):8682
Nat Commun, 2024, 15(1):668
S8828 Gboxin Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.
Cell Rep, 2024, 43(10):114775
Mol Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
S8943 VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Cancers (Basel), 2022, 14(13)3225
S0096 S-Gboxin S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM.
Cell Rep Med, 2024, 5(10):101757
EMBO Mol Med, 2022, 14(12):e16082
S2987 4-Methyl-2-oxovaleric acid 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity.
E4709New MS-L6 MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy.
E1139 DX3-213B DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor with IC50 of 3.6 nM, and impairs ATP generation with IC50 of 11 nM.
S9604 Lixumistat (IM156) Lixumistat (IM156), is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
bioRxiv, 2024, 2024.09.16.613317
E1149 BAY-179 BAY-179 is an excellent in vivo suitable tool with which to probe the biological relevance of complex I inhibition in cancer indications.
S5604 Diphenylamine Hydrochloride Diphenylamine (N-Phenylbenzenamine, Anilinobenzene, C.I. 10355), a derivative of aniline, is widely used as an industrial antioxidant, dye mordant and reagent and is also employed in agriculture as a fungicide and antihelmintic. Diphenylamine can inhibits oxidative phosphorylationsignificantly, although its inhibition potency was weaker than that of NSAIDs with a diphenylamine structure.
E4709New MS-L6 MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy.

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