货号 | 13624S |
使用方法 | Y-27632 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 1 mg in 312.2 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 1-10 µM for 15 min-4 hr. |
供应商 | CST |
背景 | Y-27632 is a potent and selective ATP-competitive inhibitor of Rho-associated kinases (ROCK), with Ki values of 0.22 µM and 0.30 µM for ROCK1 and ROCK2, respectively. In vitro kinase assays demonstrate that Y-27632 exhibits a 20-fold greater preference for ROCK when compared to citron kinase and protein kinase N (1). Research studies show that Y-27632 treatment of cells leads to inhibition of ROCK phosphorylation of myosin phosphatase subunit 1 (MYPT1) at both Thr853 and Thr696, with a much greater inhibition of Thr853 phosphorylation (2,3). Y-27632 selectively inhibits smooth-muscle contraction by inhibiting Ca2+ sensitization (4). Additional research indicates that Y-27632 inhibits dissociation-induced apoptosis of cultured human embryonic stem cells over numerous passages and increases cloning efficiency (5). |
存放说明 | -20C |
纯度 | >98% |
计算分子量 | 320.30 g/mol |
参考文献 | 1 . Ishizaki, T. et al. (2000) Mol Pharmacol 57, 976-83. 2 . Garton, A.J. et al. (2008) Methods Enzymol 439, 491-500. 3 . Ramachandran, C. et al. (2011) Mol Vis 17, 1877-90. 4 . Uehata, M. et al. (1997) Nature 389, 990-4. 5 . Watanabe, K. et al. (2007) Nat Biotechnol 25, 681-6. |
Western blot analysis of extracts from C2C12, 293, and NIH/3T3 cells, untreated (-) or treated with Y-27632 (10 μM, 1 hr; +), using Phospho-MYPT1 (Thr853) Antibody #4563 (upper) and MYPT1 Antibody #2634 (lower). | |
Chemical structure of Y-27632. |