Description: GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis. Target: Epigenetic Reader Domain. Smiles:...

GSK778 is a bromodomain 1 (BD1) inhibitor. It selectively inhibits BD1 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and bromodomain testis-specific protein (BRDT, IC50s = 79.43, 39.81, 39.81, and 158.49 nM, respectively, in time-resolved FRET assays) over BD2 in BRD2, BRD3, BRD4, and BRDT (IC50s = 3,162,...