BAY 87-2243 potently inhibits HIF-1 reporter gene activity (IC50 = 0.7 nM) and CA9 protein expression (IC50 = 2.0 nM). It strongly inhibits mitochondrial complex I activity (IC50 = 10 nM in PC3 cell mitochondria), leading to its HIF-1 effects, without affecting complex III.
| 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 |
|---|---|
| Purity | >98% |
| CAS Number | 1227158-85-1 |
| Formula | C26H26F3N7O2 |
| Molecular Weight | 525.54 |
| Appearance | Powder |
| Solubility | Dissolves in DMSO (up to 25 mg/mL) or in ethanol (up to 10 mg/mL) |
| Stability | ≥ 1 year |
| Application Procedures | First, dissolve in DMSO (up to 25 mg/mL) or in Ethanol (up to 10 mg/mL), and then dilute it into an aqueous buffer. Solutions in DMSO or ethanol can be stored at -20° for up to 2 months. |
| Storage Information | Room Temperature |
HIF-1 / Mitochondrial complex I inhibitor
Datasheet