GSK4027 is a p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain inhibitor (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).1 It is greater than 18,000-fold selective for PCAF and GCN5 over BET family bromodomains and greater than 70-fold selective over other bromodomain families in a BROMOscan assay.
1.Humphreys, P.G., Bamborough, P., Chung, C.W., et al.Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probeJ. Med. Chem.60(2)695-709(2017)
















