-
-
Overview
-
Please contact us at for specific academic pricing.
Background
BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation [1].In HCT-116 cells, BAY 87-2243 inhibits the hypoxia increased HRE-dependent luciferase expression with IC50 value of 0.7nM and inhibits the expression of HIF target gene CA9 with IC50 value of 2nM. In H460 cells cultured under hypoxia, BAY 87-2243 suppresses the expression of HIF-1 target genes including CA9, adrenomedullin and angiopoietin-like protein-4. BAY 87-2243 also inhibits both HIF-1α and HIF-2α protein accumulation in this cell line. Moreover, in mice model bearing H460 xenograft, treatment of BAY 87-2243 reduces the expression levels of HIF-1 target genes CA9, ANGPTL4 and EGLN3 and meanwhile reduces the tumor weight. 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 10nM [1].
[1] Ellinghaus P, Heisler I, Unterschemmann K, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer medicine, 2013, 2(5): 611-624.
-
- Properties
-
Overview