GSK620 (GSK-620) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.1 (BRD4 BD2), 220-fold selectivity over BD1.
GSK620 significantly and dose-dependently inhibited both the arthritic score and IgG1 production in response to the immunisation in collagen-induced arthritis model in rats.
GSK620 showed similar level of efficacy to the pan-BET inhibitor I-BET151 and also dramatically reduced joint swelling, synovitis, cartilage damage, pannus formation and bone resorption.
