BAY 87-2243

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation. It inhibits HIF-1α and HIF-2α protein accumulation under hypoxic conditions in non-small cell lung cancer (NSCLC) cell line H460 but had no effect on HIF-1α protein levels induced by the hypoxia mimetics desferrioxamine or cobalt chloride. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC₅₀ value of 10 nM.