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
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