Biochem/physiol Actions
BAY 87-2243 has a therapeutic effect on ferroptosisâ€Âbased cancer, hypoxic pancreatic cancer cells.
BAY 87-2243 is an orally active oxidative phosphorylation (OxPhos) inhibitor that potently suppresses hypoxia-induced HIF-1 activation (IC50 = 0.7 nM by HCT-116-based reporter assay; 24 h 1% O2) by selectively targeting mitochondrial complex I (IC50 = 10 nM using mitochondria from PC3; no inhibition of complex III), exhibiting antiproliferation activity in cancer cultures only in the absence of glucose (IC50 ∼3 nM in H460 cultures with 10 mM galactose or lactate, >10 μM with 10 mM glucose). BAY 87-2243 selectively inhibits hypoxia-induced, but not hypoxia-independent, HIF-1α & HIF-2α upregulation and HIF-1 target genes expression in cultures (IC50 ≤10 nM/ADM, ANGPTL4, CA9 mRNA in H460 cells; IC50 = 2 nM/carbonic anhydrase 9 (CA9) protein in HCT116 cells) and effectively suppresses H460 xenograft tumor growth in mice via daily oral admiminstration in vivo (ED50 ∼2 mg/kg).
- UPC:
- 51112802
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SML2384-25MG
- CAS:
- 1227158-85-1
