Chemical Name: 5-[5-Methyl-1-[[3-(4-methylsulfonylpiperidin-1-yl)phenyl]methyl]-1,2,4-triazol-3-yl]-3-[4-(trifluoromethoxyphenyl]-1,2,4-oxadiazole
Mitochondrial Complex I Inhibitor
Molekulargewicht:
562.57
Reinheit:
>98% by HPLC NMR (Conforms)
Formulierung:
White to off-white solid
CAS Nummer:
[1570496-34-2]
Formel:
C25H25F3N6O4S
Anwendungsbeschreibung:
IACS-010759 (1570496-34-2) is a potent (IC50 = 1.1 nM isolated mouse complex I) and selective inhibitor of complex I of the mitochondrial electron transport chain (OXPHOS). IACS-010759 displayed in vivo efficacy in glycolysis-deficient glioblastoma and AML models without cytotoxicity to normal cells. The lack of cytotoxicity to normal cells, as opposed to other complex I inhibitors, is attributed to its unique binding location on complex I.2 Complex I inhibition by IACS-010759 causes an ROS-induced decrease in the endogenous PP2A inhibitor CIP2A leading to cell death.3 It has also displayed potential in various chemotherapy-resistant cancer cell lines.4-7
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