GSK620
规格
Cas Number | 2088410-46-0 |
规格或纯度 | 10mM in DMSO |
包装 | 1ml |
产品信息
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
简短描述 | 表观遗传阅读器域抑制剂 |
英文简短描述 | Epigenetic Reader Domain Inhibitors |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | GSK620 是一种泛 BD2 抑制剂,在人体全血中显示出抗炎表型,具有出色的广泛选择性、可开发性和体内口服药代动力学。 |
英文描述 |
Information GSK620 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. Targets BD2 In vitro GSK620 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 vivo GSK620 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 |