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Merck
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Key Documents

688000

Sigma-Aldrich

Y-27632

≥95% (HPLC), solid, Rho kinase inhibitor, Calbiochem

别名:

Y-27632, ROCK抑制剂,(R)-(+)-反式-N-(4-吡啶基)-4-(1-氨基乙基)-环己烷甲酰胺,2HCl,Rho激酶抑制剂VI

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About This Item

经验公式(希尔记法):
C14H21N3O · 2HCl · xH2O
分子量:
320.26 (anhydrous basis)
分類程式碼代碼:
12352200
NACRES:
NA.77

product name

Y-27632-CAS 331752-47-7-Calbiochem, Y-27632A, CAS 331752-47-7, is a cell-permeable, reversible, inhibitor of Rho kinases (Ki = 140 nM for p160ROCK). Enhances survival & cloning efficiency of ESC without affecting their pluripotency.

品質等級

化驗

≥95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
desiccated (hygroscopic)
protect from light

顏色

white

溶解度

water: 100 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

InChI

1S/C14H21N3O/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13/h6-12H,2-5,15H2,1H3,(H,16,17,18)/t10-,11?,12?/m1/s1

InChI 密鑰

IYOZTVGMEWJPKR-VOMCLLRMSA-N

一般說明

Rho相关蛋白激酶的一种高效、细胞渗透性、可逆且选择性抑制剂(针对p160ROCK的Ki= 140 nM)。还可同等高效的抑制ROCK-II。这种抑制对于ATP具有竞争性。比p160ROCKε有10至50倍更低的PKC亲和力。即使在更高的浓度(~100 µM)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。阻止凋亡并提高解离的hES细胞的存活率和克隆效率,而不会影响其多能性。用Y-27632预处理可降低脓毒症大鼠模型中肺损伤的风险。可提供5 mM(500 µg/296µl)的Y-27963(货号688001)H2O溶液和10 mM的DMSO(货号688002)溶液。
Rho相关蛋白激酶的一种高效、细胞渗透性、可逆且选择性抑制剂(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 µM)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)。阻止凋亡并提高解离的hES细胞的存活率和克隆效率,而不会影响其多能性。用Y-27632预处理可降低脓毒症大鼠模型中肺损伤的风险。

生化/生理作用

产物与ATP竞争。
可逆性:是
细胞可渗透性:具有
靶标Ki:对p160 Rho相关激酶(ROCK)为140 nM
首要靶标
p160 Rho相关蛋白激酶(ROCK)

包裝

用惰性气体包装

警告

毒性:有害(C)

重構

溶解后,等分并冷冻保存(-20°C)。储备液可在-20°C稳定6个月。

其他說明

Cinel, I., et al. 2012.J. Thorac .Dis.4, 30.
Watanabe, K., et al. 2007.Nature Biotech.25, 681.
Chitaley, K., et al. 2001.Nat. Med.7, 119.
Davies, S.P., et al. 2000.生物化学。J. 351, 95.
Narumiya, S., et al. 2000.Methods Enzymol.325, 273.
Hirose, M., et al. 1998.J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999.Science285, 895.
Uehata, M., et al. 1997.Nature389, 990.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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