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3-(4-Pyridyl)indole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
3-(4-Pyridyl)indole图片
CAS NO:7272-84-6
规格:98%
分子量:194.2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
ROCK-I inhibitor
CAS:7272-84-6
分子式:C13H10N2
分子量:194.2
纯度:98%
存储:Store at -20°C

Background:

3-(4-pyridyl)indole (Rockout) is a Rho-kinase inhibitor [1].


Rho-associated protein kinase (ROCK) belongs to a family of serine-threonine kinases mainly involved in regulating the shape and movement of cells by acting on the cytoskeleton [2].


Rockout caused decreased migration and aberrant morphology. Rockout showed no effect on phagocytosis, listeria motility or actin polymerization in permeabilized yeast. In a human melanoma cell line M2 cells that blebs constitutively in a manner that is sensitive to actin cytoskeletal perturbation, Rockout (50 μM) stopped the cell blebbing within 2 min and with washout blebbing returned to normal levels within 3 min. The IC50 of Rockout was 12 μM and it inhibited blebbing in nearly all cells at 50 μM. In B3T3 cells, treatment with 50 μM Rockout resulted in significant morphological change within 10 min [1]. At an ATP concentration of 100 μM, Rockout inhibited ROCK activity with an approximate IC50 of 25 μM. Rockout (25 μM) inhibited ROCK-II and PRK to a similar degree, and MSK-1 and PKA to a lesser extent. Rockout showed no inhibitory effect on PKCα or SAPK2a [1].


参考文献:
[1] Yarrow J C, Totsukawa G, Charras G T, et al.  Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor[J]. Chemistry & biology, 2005, 12(3): 385-395.
[2] Amano M, Fukata Y, Kaibuchi K.  Regulation and functions of Rho-associated kinase[J]. Experimental cell research, 2000, 261(1): 44-51.