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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

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