Rho激酶抑制剂IV

RHO/ROCK通路抑制剂；抑制ROCK2

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产品号 #73802_C

RHO/ROCK通路抑制剂；抑制ROCK2

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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.）。

产品说明书及文档

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Document Type

Product Name

Catalog #

Lot #

Language

Document Type

Product Information Sheet

Product Name

Rho Kinase Inhibitor IV (Dihydrochloride)

Catalog #

73804, 73802

Lot #

All

Language

English

Document Type

Safety Data Sheet

Product Name

Rho Kinase Inhibitor IV (Dihydrochloride)

Catalog #

73804, 73802

Lot #

All

Language

English

Abstract

The derivation of astrocytes from human pluripotent stem cells is currently slow and inefficient. We demonstrate that overexpression of the transcription factors SOX9 and NFIB in human pluripotent stem cells rapidly and efficiently yields homogeneous populations of induced astrocytes. In our study these cells exhibited molecular and functional properties resembling those of adult human astrocytes and were deemed suitable for disease modeling. Our method provides new possibilities for the study of human astrocytes in health and disease.

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Chemical Interrogation of the Neuronal Kinome Using a Primary Cell-Based Screening Assay Al-Ali H et al. ACS Chemical Biology 2013 MAY

Abstract

A fundamental impediment to functional recovery from spinal cord injury (SCI) and traumatic brain injury is the lack of sufficient axonal regeneration in the adult central nervous system. There is thus a need to develop agents that can stimulate axon growth to re-establish severed connections. Given the critical role played by protein kinases in regulating axon growth and the potential for pharmacological intervention, small molecule protein kinase inhibitors present a promising therapeutic strategy. Here, we report a robust cell-based phenotypic assay, utilizing primary rat hippocampal neurons, for identifying small molecule kinase inhibitors that promote neurite growth. The assay is highly reliable and suitable for medium-throughput screening, as indicated by its Z'-factor of 0.73. A focused structurally diverse library of protein kinase inhibitors was screened, revealing several compound groups with the ability to strongly and consistently promote neurite growth. The best performing bioassay hit robustly and consistently promoted axon growth in a postnatal cortical slice culture assay. This study can serve as a jumping-off point for structure activity relationship (SAR) and other drug discovery approaches toward the development of drugs for treating SCI and related neurological pathologies.

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Applications for ROCK kinase inhibition. Al-Ali H et al. 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.

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更多信息
Molecular Weight	449.4 g/mol
种属	Human, Mouse, Non-Human Primate, Other, Rat
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