EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72302_C
RHO/ROCK 信号通路抑制剂；抑制 ROCK1 和 ROCK2
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总览
Y-27632是一种具有细胞通透性、效力强且选择性高的的ho 相关卷曲-螺旋结构蛋白激酶（ROCK）抑制剂。Y-27632 通过与 ATP 竞争结合催化位点来抑制 ROCK1 (Ki = 220 nM) 和 ROCK2 (Ki = 300 nM) (Davies 等；Ishizaki 等)。
维持与自我更新
·通过防止解离诱导的细胞凋亡（anoikis），提高人胚胎干细胞（ES）分离为单细胞后的存活率，从而提高其克隆效率（Watanabe等）。
·在强制聚集法中促进拟胚体的形成（Ungrin等）。
·提高冻存单细胞人 ES 细胞在复苏后的存活率（Li等）。
·小鼠 ES 细胞来源的神经前体细胞在解离及移植后的凋亡（Koyanagi等）。
重编程
·与 CHIR99021、RepSox、Forskolin、SP600125、Gö6983 和丙戊酸联合使用，将成纤维细胞直接谱系重编程为成熟神经元（Hu 等）。
分化
·在分化起始阶段提高人胚胎干细胞单层细胞的存活率（Rezania等）。
别名
ROCK i抑制剂
细胞类型
神经元，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化，扩增，培养，重编程，球状体培养
研究领域
干细胞生物学
CAS 编号
129830-38-2
化学式
C₁₄H₂₁N₃O · 2HCl
分子量
320.3 g/mol
纯度
≥98%
通路
RHO/ROCK
靶点
ROCK1，ROCK2
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
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相关材料与文献
技术资料 (5)
文献 (14)
Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.
Molecular pharmacology 2000 MAY
Abstract
Y-27632 [(+)-(R)-trans-4-(1-aminoethyl)-N-(4-pyridyl)cyclohexanecarboxamide++ + dihydrochloride] is widely used as a specific inhibitor of the Rho-associated coiled-coil forming protein serine/threonine kinase (ROCK) family of protein kinases. This study examined the inhibition mechanism and profile of actions of Y-27632 and a related compound,Y-30141 [(+)-(R)-trans- 4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)cyclohexan-ecarboxamide dihydrochloride]. Y-27632 and Y-30141 inhibited the kinase activity of both ROCK-I and ROCK-II in vitro,and this inhibition was reversed by ATP in a competitive manner. This suggests that these compounds inhibit the kinases by binding to the catalytic site. Their affinities for ROCK kinases as determined by K(i) values were at least 20 to 30 times higher than those for two other Rho effector kinases,citron kinase and protein kinase PKN. [(3)H]Y-30141 was taken up by cells in a temperature- and time-dependent and saturable manner,and this uptake was competed with unlabeled Y-27632. No concentrated accumulation was found,suggesting that the uptake is a carrier-mediated facilitated diffusion. Y-27632 abolished stress fibers in Swiss 3T3 cells at 10 microM,but the G(1)-S phase transition of the cell cycle and cytokinesis were little affected at this concentration. Y-30141 was 10 times more potent than Y-27632 in inhibiting the kinase activity and stress fiber formation,and it caused significant delay in the G(1)-S transition and inhibition of cytokinesis at 10 microM.
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
The Biochemical journal 2000 OCT
Abstract
The specificities of 28 commercially available compounds reported to be relatively selective inhibitors of particular serine/threonine-specific protein kinases have been examined against a large panel of protein kinases. The compounds KT 5720,Rottlerin and quercetin were found to inhibit many protein kinases,sometimes much more potently than their presumed targets,and conclusions drawn from their use in cell-based experiments are likely to be erroneous. Ro 318220 and related bisindoylmaleimides,as well as H89,HA1077 and Y 27632,were more selective inhibitors,but still inhibited two or more protein kinases with similar potency. LY 294002 was found to inhibit casein kinase-2 with similar potency to phosphoinositide (phosphatidylinositol) 3-kinase. The compounds with the most impressive selectivity profiles were KN62,PD 98059,U0126,PD 184352,rapamycin,wortmannin,SB 203580 and SB 202190. U0126 and PD 184352,like PD 98059,were found to block the mitogen-activated protein kinase (MAPK) cascade in cell-based assays by preventing the activation of MAPK kinase (MKK1),and not by inhibiting MKK1 activity directly. Apart from rapamycin and PD 184352,even the most selective inhibitors affected at least one additional protein kinase. Our results demonstrate that the specificities of protein kinase inhibitors cannot be assessed simply by studying their effect on kinases that are closely related in primary structure. We propose guidelines for the use of protein kinase inhibitors in cell-based assays.
A ROCK inhibitor permits survival of dissociated human embryonic stem cells.
ACS chemical biology 2013 MAY
Abstract
Poor survival of human embryonic stem (hES) cells after cell dissociation is an obstacle to research,hindering manipulations such as subcloning. Here we show that application of a selective Rho-associated kinase (ROCK) inhibitor,Y-27632,to hES cells markedly diminishes dissociation-induced apoptosis,increases cloning efficiency (from approximately 1% to approximately 27%) and facilitates subcloning after gene transfer. Furthermore,dissociated hES cells treated with Y-27632 are protected from apoptosis even in serum-free suspension (SFEB) culture and form floating aggregates. We demonstrate that the protective ability of Y-27632 enables SFEB-cultured hES cells to survive and differentiate into Bf1(+) cortical and basal telencephalic progenitors,as do SFEB-cultured mouse ES cells.
更多信息
| Molecular Weight | 320.3 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | ROCK inhibitor |
| Cas Number | 129830-38-2 |
| Chemical Formula | C₁₄H₂₁N₃O · 2HCl |
| 纯度 | ≥ 98% |
| Target | ROCK1, ROCK2 |
| Pathway | RHO/ROCK |
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产品仅供研究使用，不用于针对人或动物的诊断或治疗。
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
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