Background:

PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain.Target: CREBin vitro: PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 downregulates RGS4 in neurons, a target linked to Parkinson’s disease. PF-CBP1 is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC. F-CBP1 is also a potent inhibitor of EP300 (a result observed for other CBP inhibitors. [1]

[1]. Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. Chem Biol. 2015 Dec 17;22(12):1588-96.