BAY 87-2243 (BAY87-2243) is a highly potent, selective inhibitor of HIF-1, inhibits hypoxia-induced gene activation (IC50=0.7 nM), directly inhibits mitochondrial complex I.
BAY 87-2243 inhibits hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells with IC50 of 2 nM.
BAY 87-2243 inhibits hypoxia-inducible factor (HIF-1α) and HIF-2α protein accumulation in hypoxic H460 cells H460 under hypoxia, but has no effect on HIF-1α protein levels induced by hypoxia mimetics and has no effect on prolyl hydroxylase 2 (PHD2) activity.
BAY 87-2243 suppresses HIF target gene expression in hypoxic lung cancer cells.
BAY 87-2243 inhibits mitochondrial oxygen consumption with IC50 of 10 nM.
BAY 87-2243 potently inhibits cell proliferation of H460 cells with EC50 of 3 nM.
BAY 87-2243 reduces tumor weight, HIF-1α protein, and HIF-1 target gene expression levels in H460 xenograft mouse model.