GSK620
BD2 selective BET inhibitor / BET inhibitor 220-fold more selective for BD2 over BD1 (pIC50 BD2 = 7.1; BD1 = 4.8).1 It ameliorated collagen-induced arthritis in a rat model and imiquimod-induced psoriasis in a mouse model.2 GSK620 was also able to reduce hepatic fibrosis, steatosis, and inflammation in a mouse model of non-alcoholic steatohepatitis (NASH).
Biochemicals & reagents
2088410-46-0
1 Seal et al. (2020), The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor; J. Med. Chem., 63 9093 2 Gilan et al. (2020), Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation; Science, 368 387
-20°C
TARGET: Bromodomain -- PATHWAY: Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Inflammation