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/ ROCK / GSK269962A HCl

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

货号：A105790 同义名： GSK269962 hydrochloride; GSK269962B

GSK269962A HCl是一种选择性的 ROCK（Rho 相关蛋白激酶）抑制剂，对 ROCK1 和 ROCK2 的 IC50 值分别为 1.6 nM 和 4 nM。

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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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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 HCl ++++

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, IC50: 60 nM

ROCK2, Ki: 41 nM

 		99%+
Y-27632 2HCl ++

ROCK1, Ki: 140 nM

 		+

ROCK2, Ki: 300 nM

 		99%+
Fasudil HCl +

ROCK2, Ki: 330 nM

 		PKG,Rho 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 95%
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 细胞实验

Cell Line
Concentration Treated Time Description References
OCI-AML3 80 nM 72 hours Inhibited AML cell growth, induced G2 phase arrest and apoptosis Front Pharmacol. 2022 Dec 6;13:1064470.
MV4-11 80 nM 72 hours Inhibited AML cell growth, induced G2 phase arrest and apoptosis Front Pharmacol. 2022 Dec 6;13:1064470.
LepR+ MSCs 1 μM 48 hours Inhibition of ROCK1 signaling pathway, reducing the expression of fibrosis markers Col1a1, vimentin, and α-SMA Cell Commun Signal. 2024 May 6;22(1):257.
UACC62 625nM 48 hours To evaluate the effect of GSK269962A on the proliferation of MAPKi-resistant melanoma cells, showing complete inhibition of proliferation at 625nM concentration. bioRxiv [Preprint]. 2024 Jan 11:2024.01.09.574940.
M481 625nM 48 hours To evaluate the effect of GSK269962A on the proliferation of MAPKi-resistant melanoma cells, showing complete inhibition of proliferation at 625nM concentration. bioRxiv [Preprint]. 2024 Jan 11:2024.01.09.574940.
A375 625nM 48 hours To evaluate the effect of GSK269962A on the proliferation of MAPKi-resistant melanoma cells, showing complete inhibition of proliferation at 625nM concentration. bioRxiv [Preprint]. 2024 Jan 11:2024.01.09.574940.

GSK269962A HCl 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NOD-SCID/IL2Rgnull mice AML model Intraperitoneal injection 5 mg/kg and 10 mg/kg 5 days per week for 4 weeks Significantly prolonged mouse survival and reduced leukemia cell infiltration Front Pharmacol. 2022 Dec 6;13:1064470.
Mice PE-induced prostatic hyperplasia model Intraperitoneal injection 5 mg/kg Four times a week for four weeks GSK269962A reduces prostatic stromal hyperplasia and collagen deposition by inhibiting ROCK1 signaling pathway Cell Commun Signal. 2024 May 6;22(1):257.

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
SMILES Code O=C(NC1=CC=CC(OC2=CC3=C(N=C(C4=NON=C4N)N3CC)C=N2)=C1)C5=CC=C(OCCN6CCOCC6)C=C5.[H]Cl
MDL No. MFCD31536773
别名 GSK269962 hydrochloride; GSK269962B; GSK269962; GSK269962A hydrochloride; GSK 269962 hydrochloride
运输蓝冰
InChI Key UYKVMFKKKLLDGL-UHFFFAOYSA-N
Pubchem ID 57398146
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

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 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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