BAZ2A/B are bromodomain-containing proteins whose biological function 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. BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen). It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 μM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2. See the Structural Genomics Consortium (SGC) website for more information.
[1]. chen p, chaikuad a, bamborough p, et al. discovery and characterization of gsk2801, a selective chemical probe for the bromodomains baz2a and baz2b. journal of medicinal chemistry, 2015.
