GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe inhibitor of PCAF/GCN5 bromodomain with pKi of 8.9 for both.
GSK4027 displays exceptional selectivity over the BET bromodomain family (>18000-fold selectivity over the BET family, >70-fold selectivity over the wider bromodomain families) and proof of cellular target engagement.
GSK4027 is a useful chemical tool in elucidating the biological phenotype of PCAF/GCN5 bromodomain inhibition.
