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GSK429286A {[allProObj[0].p_purity_real_show]}

货号:A569516 同义名: RHO-15

GSK429286A selectively inhibits ROCK1 and ROCK2 with the IC50 value of 14 nM and 63 nM, respectively.

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GSK429286A 化学结构 CAS号:864082-47-3
GSK429286A 化学结构
CAS号:864082-47-3
GSK429286A 3D分子结构
CAS号:864082-47-3
GSK429286A 化学结构 CAS号:864082-47-3
GSK429286A 3D分子结构 CAS号:864082-47-3
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GSK429286A 纯度/质量文件 产品仅供科研

货号:A569516 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ROCK ROCK1 ROCK2 其他靶点 纯度
Thiazovivin +

ROCK, IC50: ~0.5 μM

98%
Netarsudil hydrochloride ++++

ROCK, Ki: 2 nM

99%+
Y-33075 2HCl ++++

ROCK, IC50: 3.6 nM

99%+
ROCK1-IN-1 ++

ROCK, Ki: 17nM

95%
GSK429286A +++

ROCK1, IC50: 14 nM

++

ROCK2, IC50: 63 nM

99%+
Ripasudil ++

ROCK1, IC50: 51 nM

++

ROCK2, IC50: 19 nM

99%+
Belumosudil ++

ROCK2, Ki: 41 nM

ROCK2, IC50: 60 nM

99%+
Y-27632 dihydrochloride ++

ROCK1, Ki: 140 nM

+

ROCK2, Ki: 300 nM

99%+
Fasudil HCl +

ROCK2, Ki: 330 nM

Rho,PKG 98%
Chroman 1 ++++

ROCK1, IC50: 52 pM

++++

ROCK2, IC50: 1 pM

99%
BAY-549 ++++

ROCK1, IC50: 0.6 nM

++++

ROCK2, IC50: 1.1 nM

99%+
AT13148 +++

ROCK1, IC50: 6 nM

+++

ROCK2, IC50: 4 nM

PKA 98+%
RKI-1447 +++

ROCK1, IC50: 14.5 nM

+++

ROCK2, IC50: 6.2 nM

99%+
Hydroxyfasudil HCl +

ROCK1, IC50: 0.73 μM

+

ROCK2, IC50: 0.72 μM

PKA 98%
H-1152 2HCl +++

ROCK2, IC50: 0.0120 μM

PKG 99%
GSK269962A HCl ++++

ROCK1, IC50: 1.6 nM

+++

ROCK2, IC50: 4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GSK429286A 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.

GSK429286A 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 expressed in Sf9 cells at 10 mM, IC50=0.014 μM 17201405

GSK429286A 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.

GSK429286A 实验方案

计算器
存储液制备 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

GSK429286A 技术信息

CAS号864082-47-3
分子式C21H16F4N4O2
分子量 432.371
别名 RHO-15
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

动物实验配方

15% Captisol++water 15 mg/mL suspension

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