BAY 87-2243 | HIF-1 / Mitochondrial complex I inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $235.00 |
BAY 87-2243 (1227158-85-1) 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
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
BAY 87-2243 (1227158-85-1) 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
References/Citations:
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
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1-855-FOCUS21
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