GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC 50 values of 6.0 and 4.3 for BRPF1 and BRPF2 , respectively
In Vitro
GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrates properties suitable for cellular and in vivo studies. GSK6853 is a less active analogue of GSK6853 in which the 5-amide is alkylated. MCE has not independently confirmed the accuracy of these methods. They are for reference only.