GSK620 Is an orally active, potent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 6.5/4.6/BRD2, 7.1/4.6/BRD3, 7.1/4.8/BRD4, 6.7/4.6/BRDT) with improved oral availability than GSK046 (iBET-BD2) and in vivo efficacy in inflammatory disease models, including collagen-induced arthritis (3-10 mg/kg/d p.o. in rats), imiquimod (IMQ)-induced psoriasis (20 mg/kg/d p.o. in mice), and a nonalcoholic steatohepatitis (NAFLD) model (20 mg/kg/d p.o. in STAM mice).
Potent and selective pan-second bromodomain (BD2) inhibitor with in vivo efficacy in inflammatory disease models and improved oral availability than GSK046.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Listings
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