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GSK620
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK620图片
CAS NO:2088410-46-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
GSK620 是一种有效的口服活性泛 BD2 抑制剂,具有良好的广谱选择性、可开发性和体内口服药代动力学,对 BET-BD2 家族蛋白具有高度选择性,其选择性超过所有其他 BET bromodomains 200 倍以上。GSK620 在人全血中表现出抗炎表型。
Cas No.2088410-46-0
分子式C18H19N3O3
分子量325.36
溶解度DMSO : 62.5 mg/mL (192.09 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood[1].

GSK620 shows an anti-inflammatory phenotype in human whole blood. Human blood samples are stimulated with LPS, which produces a strong immune response. The monocyte chemattractant protein 1 (MCP-1/CCL2) is measured. This is a chemokine which recruits monocytes, memory T cells, and dendritic cells to sites of inflammation. GSK620 reduces the MCP-1 response in a concentration-dependent manner with (an expected) ∼1 log drop off in potency relative to the biochemical BRD4 BD2 potencies observed[1].

Highlighting the utility of GSK620 as an in vivo tool, efficacy is observed in separate models of inflammatory arthritis, psoriasis, and hepatitis[1].

[1]. Seal JT, et al. 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. 2020;63(17):9093-9126.