您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Rhosin
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Rhosin
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。
Rhosin图片
CAS NO:1173671-63-0
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议

产品介绍
Rhosin是Rho特异性抑制剂,结合WTRhoA的Kd值为0.4uM,对Cdc42和Rac1作用无。
Cas No.1173671-63-0
Canonical SMILESO=C(N/N=C/C1=CC=C2N=CC=NC2=C1)[C@H](N)CC3=CNC4=C3C=CC=C4
分子式C20H18N6O
分子量358.4
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Rhosin is a specific Rho inhibitor; binds to WT RhoA with an affinity ~0.4 uM Kd; does not interfere with the binding of Cdc42 or Rac1.IC50 value: 0.4 uM(binding Kd) [1]Target: RhoA inhibitorRhosin is specific to the interaction between RhoA and its GEFs including LARG, DBL, LBC, p115 RhoGEF or PDZ RhoGEF and does not interfere with the binding of Cdc42 or Rac1 to their respective GEFs. Rhosin showed a dose-dependent inhibition of endogenous RhoA activity and cell growth of MCF7 cells. Rhosin dose-dependently reduced RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50μM, and caused decreased size and reduced number of mammospheres in MCF7 cells [1]. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions [2].

[1]. Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. [2]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.