BAY 87-2243
HIF-1 / Mitochondrial complex I inhibitor / 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-1α and HIF-2α 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
Biochemicals & reagents
1227158-85-1
1) Ellinghaus et al. (2013), BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I; Cancer Med.,2 611 2) Schockel et al. (2015), Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth; Cancer Metab., 3 11 3) Basit et al. (2017), Mitochondrial complex I inhibition triggers a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis in melanoma cells; Cell Death Discov., 8 e2716
RT
TARGET: Transcription factor -- PATHWAY: Redox; Transcription; Mitochondrial function; Ferroptosis; NAD, NADP pathways; Mitophagy -- RESEARCH AREA: Oxidative stress; Cell death -- DISEASE AREA: Cancer