CCG 50014 |
| カタログ番号GC16846 |
CCG 50014 は、G タンパク質シグナル伝達タンパク質タイプ 4 (RGS4) の調節因子に対して最も強力であり (IC50 = 30 nM)、他の RGS タンパク質よりも RGS4 に対して >20 倍選択的です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 883050-24-6
Sample solution is provided at 25 µL, 10mM.
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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.
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