EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #73802_C
RHO/ROCK通路抑制剂；抑制ROCK2
若您需要咨询产品或有任何技术问题，请通过官方电话 400 885 9050 或邮箱 info.cn@stemcell.com 与我们联系。
总览
Rho激酶抑制剂IV是一种选择性和强效的Rho相关卷曲螺旋蛋白激酶2抑制剂 (ROCK2；IC₅₀= 11.8 nM；Tamura et al.)。它是法舒地尔（产品号 #73662）的甘氨酰类似物，对ROCK2 （Tamura）具有更高的特异性。Rho激酶抑制剂IV比其他ROCK抑制剂更强效，包括Y-27632 （Ki = 220 nM）和法舒地尔（IC₅₀= 158 nM）。与其他激酶相比，它对ROCK2表现出良好的特异性，例如钙/钙调蛋白依赖性激酶II型（IC₅₀= 2.57 μM）、PKG (IC₅₀= 2.35 μM),、Aurora A （IC₅₀= 3.26 μM）或PKA或PKC （IC₅₀各 ≥ 10 μM）。ROCK1和ROCK2作用于G蛋白Rho的下游，调节肌动蛋白-肌球蛋白的周转和动态，在干细胞更新、平滑肌收缩、细胞粘附和增殖中发挥重要作用(Narumiya et al.; Olson; Watanabe et al.)。本产品以5mg /mL的甲醇溶液形式提供。
分化
·促进大鼠原代神经元培养中的神经突生长（Al-Ali et al.）。
·抑制非洲爪蟾胚胎中原始肠管的发育，包括中肠伸长（Reed et al.）。
疾病建模
·降低兔青光眼模型的眼压（Tamura et al.）。
别名
(S)-甘氨酰-H-1152
细胞类型
肠道细胞，神经元
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化
研究领域
疾病建模，神经科学，干细胞生物学
CAS 编号
Rho激酶抑制剂IV：913844-45-8，甲醇：67-56-1
化学式
C₁₈H₂₄N₄O₃S · 2HCl
分子量
449.4 g/mol
纯度
≥98%
通路
RHO/ROCK
靶点
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。
相关材料与文献
文献 (7)
文献 (7)
Development of specific Rho-kinase inhibitors and their clinical application.
ACS chemical biology 2013 MAY
Abstract
Hexahydro-1-(isoquinoline-5-sulfonyl)-1H-1,4-diazepine,HA-1077,is a known selective inhibitor of Rho-kinase. Although its IC(50) value against Rho-kinase is more than 10 times lower than those for kinases such as PKA,PKB,PKC,PKG,MLCK,CaMKII and others,the molecule still retains relative potent inhibition activities against these kinases. In order to produce highly specific Rho-kinase inhibitors,several HA-1077 analogs were synthesized and their kinase inhibition properties evaluated. (S)-Hexahydro-1-(4-ethenylisoquinoline-5-sulfonyl)-2-methyl-1H-1,4-diazepine was found to be a potent Rho-kinase inhibitor. The IC50 value against Rho-kinase was 6 nM,while those against other kinases remained at almost the same level as that of HA-1077. Furthermore,we designed HA-1077 analogs on the basis of the complex structure of PKA and HA-1077. Amongst these,(S)-hexahydro-4-glycyl-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1H-1,4-diazepine and other glycine derivatives were found to be highly specific Rho-kinase inhibitors. These Rho-kinase specific inhibitors were applied to rabbit ocular hypertensive models and were shown to reduce intraocular pressure. These results demonstrate that the new 5-isoquinolinesulfonylamides are not only potent ROCK selective compounds,but are also useful compounds for clinical applications.
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.
Applications for ROCK kinase inhibition.
ACS chemical biology 2013 MAY
Abstract
ROCK kinases,which play central roles in the organization of the actin cytoskeleton,are tantalizing targets for the treatment of human diseases. Deletion of ROCK I in mice revealed a role in the pathophysiological responses to high blood pressure,and validated ROCK inhibition for the treatment of specific types of cardiovascular disease. To date,the only ROCK inhibitor employed clinically in humans is fasudil,which has been used safely in Japan since 1995 for the treatment of cerebral vasospasm. Clinical trials,mostly focusing on the cardiovascular system,have uncovered beneficial effects of fasudil for additional indications. Intriguing recent findings also suggest significant potential for ROCK inhibitors in the production and implantation of stem cells for disease therapies.
更多信息
| Molecular Weight | 449.4 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | (S)-Glycyl-H-1152 |
| Cas Number | Rho Kinase Inhibitor IV: 913844-45-8, Methanol: 67-56-1 |
| Chemical Formula | C₁₈H₂₄N₄O₃S · 2HCl |
| 纯度 | ≥ 98% |
| Target | ROCK2 |
| Pathway | RHO/ROCK |
相关产品
-
NeuroCult™ 基础培养基（小鼠和大鼠）小鼠和大鼠神经干祖细胞培养的基础培养基
-
NeuroCult™ NS-A 扩增试剂盒（人）培养人神经干细胞和祖细胞的培养基
-
ThiazovivinRHO/ROCK 通路抑制剂；抑制 ROCK
-
Y-27632（二盐酸盐）RHO/ROCK 信号通路抑制剂；抑制 ROCK1 和 ROCK2
质量保证:
产品仅供研究使用，不用于针对人或动物的诊断或治疗。 Safety Statement: CA WARNING: This product can expose you to Methanol which is known to the State of California to cause birth defects or other reproductive harm. For more information go to www.P65Warnings.ca.gov
产品仅供研究使用，不用于针对人或动物的诊断或治疗。 Safety Statement: CA WARNING: This product can expose you to Methanol which is known to the State of California to cause birth defects or other reproductive harm. For more information go to www.P65Warnings.ca.gov
沪公网安备31010102008431号
在线联系