BAY 87-2243

BAY 87-2243

Biochem/physiol Actions

BAY 87-2243 has a therapeutic effect on ferroptosis?based 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).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576240 BAY 87-2243 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£469.39 (exc VAT) per 25MG
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3576241 BAY 87-2243 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£116.16 (exc VAT) per 5MG
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