GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
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[1].
[1]. Bamborough P, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7.
















