推荐产品
产品名称
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.
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
white
溶解性
water: 100 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
N[C@@H](C1CCC(CC1)C(=O)Nc2ccncc2)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 key
IYOZTVGMEWJPKR-VOMCLLRMSA-N
一般描述
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）
p160 Rho相关蛋白激酶（ROCK）
包装
用惰性气体包装
警告
毒性：有害（C）
重悬
溶解后，等分并冷冻保存（-20°C）。储备液可在-20°C稳定6个月。
其他说明
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.
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
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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