纯度:>98% by HPLC;NMR (Conforms)
分子式:C25H25F3N6O4S
分子量:562.57
溶剂:DMSO (>25 mg/ml)
性状:White to off-white solid
存储:-20°C
Activity (short version):Mitochondrial Complex I Inhibitor
Function / Pharmacology: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