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CCG 50014
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。
CCG 50014图片
CAS NO:883050-24-6
规格:98%
分子量:316.35
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
RGS4 Inhibitor,potent and selective
CAS:883050-24-6
分子式:C16H13FN2O2S
分子量:316.35
纯度:98%
存储:Store at -20°C

Background:

CCG-50014 is a potent and small molecule RGS inhibitor (IC50= 30 nM for RGS4, more than 20 fold selectivity for RGS4 over other RGS proteins). It is a GTPase activating protein that binds to the Gα –subunits of activated heterotrimeric G-proteins and boost GTP hydrolysis rate. [1][2]


RGS (regulator of G protein signaling) inactivates G proteins by promoting GTPase hydrolysis ability of the alphas subunit, thus inhibits the G protein signaling transduction.


In living HEK293T cells, CCG-50014 inhibited Gαo-dependent membrane translocation of GFP-RGS4. HEK293T cell transfected with GFP-RGS4 and Gαo with vehicle (0.1% DMSO) did not changed the membrane localization of RGS4, CCG-50014 (100 μM) reversed the membrane localization of RGS. [1]


参考文献:
[1] Blazer LL, Zhang H, Casey EM et al.  A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry. 2011 Apr 19;50(15):3181-92.
[2] Vashisth H, Storaska AJ, Neubig RR et al.  Conformational dynamics of a regulator of G-protein signaling protein reveals a mechanism of allosteric inhibition by a small molecule. ACS Chem Biol. 2013 Dec 20;8(12):2778-84.