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) |
水 |
<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 |
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