GSK180736ACAS号： 817194-38-0分子式： C19H16FN5O2分子量： 365.13描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)参考文献
| 产品描述 | |
| 描述 |
GSK180736A是一种Rho相关的、含卷曲螺旋（coiled-coil）的蛋白激酶抑制剂，与GRK2(G protein-coupled receptor kinase 2)结合，logIC50为-6.6。对GRK2的选择性比对GRK1和GRK5高400倍以上。 |
| 纯度 |
99%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 外观 |
powder
|
| 可溶性/溶解性 |
DMSO：73 mg/mL warmed (199.8 mM)
Ethanol：3 mg/mL warmed (8.21 mM) |
| 生物活性 | |
| 靶点 |
ROCK ,GRK2
|
| In vitro(体外研究) |
GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).
|
| 参考文献 | |
| 参考文献 |
[1]、Waldschmidt HV, et al. Structure-Based Design, Synthesis and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 6.
|
分子结构图
