产品名称
Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases
assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
shipped in
wet ice
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
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
Disclaimer
毒性:有害(C)
General description
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)。
Legal Information
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
Other Notes
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.
Packaging
用惰性气体包装
Physical form
5 mM (500 µg/296 µl)Y-27632(目录号688000)的H₂O溶液。
Preparation Note
初次融化后,等分并冷冻(-20°C)。
存储类别
12 - Non Combustible Liquids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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