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GSK269962A HCl {[allProObj[0].p_purity_real_show]}

货号：A105790 同义名： GSK269962 hydrochloride;GSK269962B

GSK269962 HCl is a selective ROCK (Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

GSK269962A HCl 化学结构 CAS号：2095432-71-4
GSK269962A HCl 化学结构
CAS号：2095432-71-4
GSK269962A HCl 3D分子结构
CAS号：2095432-71-4
GSK269962A HCl 化学结构 CAS号：2095432-71-4
GSK269962A HCl 3D分子结构 CAS号：2095432-71-4
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GSK269962A HCl 纯度/质量文件 产品仅供科研

货号：A105790 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

GSK269962A HCl 生物活性

靶点

  • ROCK1

    ROCK1, IC50:1.6 nM

  • ROCK2

    ROCK2, IC50:4 nM
描述 GSK269962A (GSK 269962) is a potent ROCK inhibitor, which effective against both ROCK1 and ROCK2 isoforms, with IC50 values of 1.6 and 4 nM, respectively. GSK269962A has anti-inflammatory and vasodilatory activities[1].
体内研究

GSK269962A, administered via oral gavage at doses of 0.3, 1, and 3 mg/kg, leads to a dose-dependent and significant reduction in blood pressure in spontaneously hypertensive rats (SHR), indicating its potential in managing hypertension[1].
体外研究

GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM[1].

GSK269962A HCl 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM SANGER
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM SANGER
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM SANGER
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM SANGER

GSK269962A HCl 动物研究

Dose Rat: 30 mg/kg[2] (i.v.); 1 mg/kg- 30 mg/kg[3] (p.o.); 5 mg/kg, 10 mg/kg[4] (intra-arterially)
Administration i.v., p.o., intra-arterially

GSK269962A HCl 参考文献

[1]Doe C, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.

GSK269962A HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.24mL

1.65mL

0.82mL

16.47mL

3.29mL

1.65mL

GSK269962A HCl 技术信息

CAS号2095432-71-4
分子式C29H31ClN8O5
分子量 607.06
别名 GSK269962 hydrochloride;GSK269962B;GSK269962;GSK269962A hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度
动物实验配方

IP 2% DMSO+water 0.7 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: GSK269962A | 2095432-71-4 | GSK 269962 | GSK269962 | GSK-269962 | ROCK Inhibitor | Cell Cycle/DNA Damage | TGF-beta/Smad | Stem Cell/Wnt | Cytoskeleton | ROCK | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GSK269962A HCl 纯度/质量文件 | GSK269962A HCl 亚型比较 | GSK269962A HCl 生物活性 | GSK269962A HCl 细胞研究 | GSK269962A HCl 动物研究 | GSK269962A HCl 参考文献 | GSK269962A HCl 实验方案 | GSK269962A HCl 技术信息

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