BAY 87-2243, HIF-1 / Mitochondrial complex I inhibitor (TBI4910)

Description

Product Details

Formal 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 Formula: C₂₆H₂₆F₃N₇O₂

Formula Weight: 525.54

CAS Number: 1227158-85-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml)

Storage: RT

Stability: ≥ 1 year.

Applications

HIF-1 / Mitochondrial complex I inhibitor

Functions

Potently inhibits HIF-1 reporter gene activity (IC50 = 0.7 nM) and CA9 protein expression (IC50 = 2.0 nM). Blocked 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 strongly 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. Reduces melanoma tumor growth via its targeting of mitochondrial complex I.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml) or in Ethanol (up to 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.