|CCG 50014 RGS4 Inhibitor,potent and selective|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||883050-24-6||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
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. 
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. 
 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.
 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.