HIF Inhibitor V

A cell-permeable phenoxyacrylamido compound that inhibits hypoxia-induced cellular HIF-1α accumulation in a manner similar to LW6 (Cat. No. 400083) by upregulating von Hippel-Lindau tumor suppressor gene product pVHL, but with much higher potency (IC₅₀ = 120 nM vs 2.44 µM, respectively, against hypoxia-induced HRE reporter activity in HCT116 cells). Shown to suppress the mRNA levels of HIF-1 target genes in HCT116 cultures (VEGF, EPO, and MMP-9; effective conc. ≥2 µM) and effectively inhibit HUVEC tubule formation (effective conc. 2 to 5 µM) under hypoxia conditions.

A cell-permeable phenoxyacrylamido compound that inhibits hypoxia-induced cellular HIF-1α accumulation in a manner similar to LW6 (Cat. No. 400083) by upregulating Hippel-Lindau tumor suppressor gene product pVHL, but with much higher potency (IC₅₀ = 120 nM vs 2.44 µM, respectively, against hypoxia-induced HRE reporter activity in HCT116 cells). Shown to suppress HIF-1 target genes expression in HCT116 cultures and inhibit HUVEC tubule formation (effective conc. ≥2 µM) under hypoxia conditions.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

Naik, R., et al. 2012. J. Med. Chem.55, 10564.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany