GSK429286A是一种选择性 ROCK1 和 ROCK2 抑制剂,对 ROCK1 和 ROCK2 的 IC50 分别为 14 nM 和 63 nM,用于研究 Rho 相关信号通路。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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 | 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 | 99% | |||||||||||||||
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。 |
靶点 |
|
描述 | GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. |
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 |
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 |
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 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 | 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
动物实验配方 | 15% Captisol++water 15 mg/mL suspension |