4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile

Description

BAZ2A/B are bromodomain-containing proteins whose biological function, while not yet confirmed, is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci. A rare allele of BAZ2B has been identified to be a predictor of Sudden Cardiac Death. BAZ2-ICR is a small molecule inhibitor of BAZ2A (K_d = 109 nM; IC₅₀ = 130 nM) and BAZ2B (K_d = 170 nM; IC₅₀ = 180 nM) bromodomains. It demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR has been shown to displace BAZ2 bromodomains in living cells by demonstrating accelerated FRAP recovery at 1 μM in the BAZ2A FRAP assay. See the Structural Genomics Consortium (SGC) website for more information.