Y-27632

Y-27632 CAS号: 146986-50-7分子式: C14H21N3O分子量: 247.34描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述

Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over Others kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

纯度
≥98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
Y 27632;Y-27632
外观
white Powder
可溶性/溶解性
DMSO : ≥ 32 mg/mL (129.38 mM)
生物活性
靶点
ROCK-I;ROCK-II;PKN;PKCα;PKA;Citron kinase
In vitro(体外研究)
Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 µM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 µM Y-27632 induced group.
In vivo(体内研究)
Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group).
参考文献
参考文献
[1]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.
[2]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5.
[3]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.
[4]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.

分子结构图

Y-27632