CCG 50014 |
| Catalog No.GC16846 |
CCG 50014는 G-단백질 신호전달 단백질 4형(RGS4)(IC50 \u003d 30nM)의 조절인자에 대해 가장 강력하고 다른 RGS 단백질에 비해 RGS4에 대해 \u003e20배 선택성입니다.
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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