CCG 50014

- Overview
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    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]
    
    [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.
- Properties
  - Alternative Name
    
    4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
    
    CAS Number
    
    883050-24-6
    
    Molecular Formula
    
    C16H13FN2O2S
    
    Molecular Weight
    
    316.35
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only