BAY 87-2243 | B1878

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation. It inhibits HIF-1α and HIF-2α protein accumulation under hypoxic conditions in non-small cell lung cancer (NSCLC) cell line H460 but had no effect on HIF-1α protein levels induced by the hypoxia mimetics desferrioxamine or cobalt chloride. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC₅₀ value of 10 nM.

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation. It inhibits HIF-1α and HIF-2α protein accumulation under hypoxic conditions in non-small cell lung cancer (NSCLC) cell line H460 but had no effect on HIF-1α protein levels induced by the hypoxia mimetics desferrioxamine or cobalt chloride

B1878 | BAY 87-2243 DataSheet

Alternate Name/Synonyms: 5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1227158-85-1

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₆H₂₆F₃N₇O₂

Molecular Weight: 525.53

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (>7 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A highly potent and selective inhibitor of hypoxia-induced gene activation.

MDL Number: N/A

PubChem CID: 67377767

SMILES: CC1=CC(=NN1CC2=CC(=NC=C2)N3CCN(CC3)C4CC4)C5=NC(=NO5)C6=CC=C(C=C6)OC(F)(F)F

InChi: InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3

InChi Key: CDJNNOJINJAXPV-UHFFFAOYSA-N