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. Author manuscript; available in PMC: 2012 Apr 19.
Published in final edited form as: Biochemistry. 2011 Mar 29;50(15):3181–3192. doi: 10.1021/bi1019622

Figure 1. The chemical structure and RGS inhibitory activity of CCG-50014.

Figure 1

A) The chemical structure of CCG-50014 (4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione). B) CCG-50014 concentration-dependently inhibits the binding between aluminum fluoride-activated Gαo and RGS4 or RGS8. Data shown are an average of three independent experiments. This experiment has been independently repeated 28 times, producing average IC50 values of 30±6 nM against RGS4 and 11±2 μM against RGS8. C,D) CCG-50014 also inhibits the GAP activity of RGS4 and E,F) RGS8. Using a single-turnover GAP assay, CCG-50014 concentration-dependently inhibits the GAP activity of both RGS4 and RGS8. * P <0.05, *** P <0.0001. All experiments were independently repeated a minimum of three times.