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GSK180736A

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Chemical Structure| 817194-38-0 同义名 : GSK180736
CAS号 : 817194-38-0
货号 : A164666
分子式 : C19H16FN5O2
纯度 : 99%+
分子量 : 365.361
MDL号 : MFCD30533616
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(82.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 GSK180736A emerges as a potent inhibitor of Rho-associated coiled-coil kinase 1 (ROCK1), exhibiting an IC50 value of 100 nM. Its action extends as a selective and ATP-competitive inhibitor of G protein-coupled receptor kinase 2 (GRK2), with an IC50 of 0.77 μM[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Sf9 cells Function assay Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA, IC50=0.014 μM 18842034
Sf9 cells 10 mM Function assay Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM, IC50=0.014 μM 17201405
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.69mL

2.74mL

1.37mL

27.37mL

5.47mL

2.74mL
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 28;59(8):3793-807.