代理GSK429286A/864082-47-3 卷曲蛋白激酶(ROCK)抑制剂,50mg 现货


产品描述 GSK429286A是一种选择性的ROCK1和ROCK2抑制剂,IC50分别为14 nM和63 nM。
靶点 ROCK1 ROCK2
IC50 14 nM[1] 63 nM[2]
体外研究 GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM.[1]GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho.[2]
体内研究 GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg.[1]
特征 More selective than Y-27632.

GSK429286A/864082-47-3 卷曲蛋白激酶(ROCK)抑制剂,50mg化学属性

溶解性 (25°C)* 体外 DMSO 87 mg/mL (201 mM)
<1 mg/mL (<1 mM)
乙醇 4 mg/mL (9 mM)
体内 15% Captisol/citrate vehicle, 15 mg/mL
*<1 mg/ml 指产品微溶或不溶*溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。
Chemical Name N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide

其他相关的 ROCK 产品:

LEE011

LEE011 是一口服有效的,高度特异性CDK4/6抑制剂。

EHop-016

EHop-016 是一种特异性的Rac GTPase抑制剂,作用于Rac1, IC50为1.1 μM,同等有效抑制Rac3。

ZCL278

ZCL278是一个选择性的Cdc42 GTP酶抑制剂,Kd为11.4 μM。

Y-27632 2HCl

Y-27632 2HCl是一种选择性的ROCK1(p160ROCK)抑制剂,Ki为140 nM,比对其他激酶包括PKC,cAMP依赖性蛋白激酶, MLCK和PAK的作用强200多倍。

Thiazovivin

Thiazovivin是一种新型ROCK抑制剂,IC50为0.5 μM,在单细胞分离后,促进人胚胎干细胞(hESC)的存活。

Fasudil (HA-1077) HCl

Fasudil (HA-1077) HCl是一种有效的ROCK-II, PKA, PKG, PKC,和MLCK抑制剂, Ki分别为0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM,和36 μM。

RKI-1447

RKI-1447是一种有效的ROCK1和ROCK2抑制剂,IC50分别为14.5 nM和6.2 nM,有抗侵入和抗肿瘤活性。

Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂,IC50为11 nM/16 nM,对CDK1/2/5, EGFR, FGFR, PDGFR, InsR等没有抑制活性。Phase 3。

特征: PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。

Alisertib (MLN8237)

Alisertib (MLN8237)是一种选择性的Aurora A抑制剂,IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Phase 3。

特征: MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。

BI 2536

BI 2536是一种有效的Plk1抑制剂,IC50为0.83 nM,比作用于Plk2和Plk3选择性分别高4和11倍。Phase 2。

特征: BI 2536是第一个有效的Plk1选择性抑制剂,抑制 Plk1的标记。

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