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Product Details

BAY 87-2243 | HIF-1 / Mitochondrial complex I inhibitor

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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Catalog#  10-4910-0005

$60.00
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CAS:
1227158-85-1
Catalog Number:
10-4910
Activity:
HIF-1 / Mitochondrial complex I inhibitor
Chemical Name:
5-[1-[[2-(4-Cyclopropylpiperazin-1-yl)pyridin-4-yl]methyl]-5-methylpyrazol-3-yl]-3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazole
Molecular Weight:
525.54
Molecular Formula:
C26H26F3N7O2
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (10 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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