| 产品描述: | 表观遗传阅读器域抑制剂;Epigenetic Reader Domain Inhibitors;;InformationGSK620 GSK620 is a pan- BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.TargetsBD2In vitroGSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 is capable of reducing the MCP-1 response in a concentration-dependent manner, providing strong evidence that GSK620 is indeed engaging BD2 in cells.In vivoGSK620 is a potent and selective pan-BD2 inhibitor with excellent in vivo PK properties and excellent developability properties, with the exception of moderate FaSSIF solubility driven by its highly crystalline nature.Cell Research(from reference)Cell lines:human whole blood, hepatocytes Concentrations:0.5 μM Incubation Time:60 min, 120 min |