推荐产品
质量水平
检测方案
≥95% (HPLC)
形式
liquid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
运输
wet ice
储存温度
−20°C
一般描述
Rho相关蛋白激酶的一种高效、细胞可渗透性、选择性抑制剂（针对p160ROCK(ROCK-I）的Ki= 140 nM）。还可几乎同等高效的抑制ROCK-II。抑制是通过与ATP竞争结合催化亚基而实现的。比p160ROCKε有10至50倍更低的PKC亲和力。即使在高浓度（~100 M）下也不影响p21激活蛋白激酶（PAK）的活性。还可作为肌球蛋白磷酸化和平滑肌收缩的激动剂诱导的Ca2+敏化的一种有效抑制剂（在主动脉环上针对苯肾上腺素诱导的收缩IC50 = 700 nM）。
可提供5 mM (500 µg/296 µl）的Y-27963(目录号 688000)的水溶液。Rho相关蛋白激酶的一种高效、细胞可渗透性、选择性抑制剂（针对p160ROCK(ROCK-I）的Ki= 140 nM）。还可几乎同等高效的抑制ROCK-II。抑制是通过与ATP竞争结合催化亚基而实现的。比p160ROCKε有10至50倍更低的PKC亲和力。即使在高浓度（~100 M）下也不影响p21激活蛋白激酶（PAK）的活性。还可作为肌球蛋白磷酸化和平滑肌收缩的激动剂诱导的Ca2+敏化的一种有效抑制剂（在主动脉环上针对苯肾上腺素诱导的收缩IC50 = 700 nM）。
生化/生理作用
主要靶标
p160ROCK
p160ROCK
产物与ATP竞争。
可逆：否
细胞渗透性：是
靶标IC50：针对苯肾上腺素诱导的主动脉条收缩为700 nM
靶标Ki：对于p160ROCK (ROCK-I)为140 nM
包装
用惰性气体包装
警告
毒性：有害（C）
外形
5 mM (500 µg/296 µl)Y-27632(目录号688000)的H₂O溶液。
重悬
初次融化后，等分并冷冻（-20°C）。
其他说明
Chitaley, K., et al. 2001.Nat. Med.7, 119.
Davies, S.P., et al. 2000.Biochem.J. 351, 95.
Narumiya, S., et al. 2000.Methods Enzymol.325, 273.
Hirose, M., et al. 1999.J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999.Science285, 895.
Uehata, M., et al. 1997.Nature389, 990.
Davies, S.P., et al. 2000.Biochem.J. 351, 95.
Narumiya, S., et al. 2000.Methods Enzymol.325, 273.
Hirose, M., et al. 1999.J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999.Science285, 895.
Uehata, M., et al. 1997.Nature389, 990.
法律信息
在PCT Application W098/06，433A1的许可和三菱制药田边分公司的许可下进行销售。
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
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