GSK429286A

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Chemical Structure| 864082-47-3 同义名 : RHO-15
CAS号 : 864082-47-3
货号 : A569516
分子式 : C21H16F4N4O2
纯度 : 99%+
分子量 : 432.37
MDL号 : MFCD16618404
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(115.64 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
生物活性
靶点

  • ROCK1

    ROCK1, IC50:14 nM

  • ROCK2

    ROCK2, IC50:63 nM
描述 GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
Sf9 cells 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

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.13mL

4.63mL

2.31mL
参考文献

[1]Nichols RJ, Dzamko N, et al. Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60.

[2]Goodman KB, Cui H, et al. Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.