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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
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
CCG 50014 对 G 蛋白信号蛋白 4 型 (RGS4) (IC50 \u003d30 nM) 的调节剂最有效，对 RGS4 的选择性比其他 RGS 蛋白高 20 倍以上。
Cas No.883050-24-6
化学名4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
Canonical SMILESCC1=CC=C(C=C1)N2C(=O)N(C(=O)S2)CC3=CC=C(C=C3)F
分子式C16H13FN2O2S
分子量316.35
溶解度DMF: 10 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL,DMSO: 10 mg/mL,Ethanol: 1 mg/mL
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

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]

References:
[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.