CCG 50014 |
| Catalog No.GC16846 |
CCG 50014 est le plus puissant contre le régulateur de la protéine de signalisation de la protéine G de type 4 (RGS4) (IC50 \u003d 30 nM) et est \u003e 20 fois sélectif pour RGS4 par rapport aux autres protéines RGS.
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.
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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