纯度:98% by HPLC;NMR (Conforms)
分子式:C26H26F3N7O2
分子量:525.54
溶剂:DMSO (25 mg/ml) Ethanol (10 mg/ml)
性状:White solid
存储:RT
Activity (short version):HIF-1 / Mitochondrial complex I inhibitor
Function / Pharmacology:BAY 87-2243 potently inhibits HIF-1 reporter gene activity (IC50 = 0.7 nM) and CA9 protein expression (IC50 = 2.0 nM).1 It inhibited HIF-1? and HIF-2? protein accumulation in hypoxic H460 cells and reduced tumor weight in nude mice inoculated with H460 cells. BAY 87-2243 potently inhibits mitochondrial complex I activity (IC50 = 10 nM in mitochondria isolated from PC3 cells) leading to its HIF-1 effects. It has no effect on mitochondrial complex III. BAY 87-2243 reduced melanoma tumor growth via its targeting of mitochondrial complex I.2,3