Table 1.
RGS | IC50 (μM) ± SEM | Hill Slope |
---|---|---|
RGS4 wild Type | 0.030 ± 0.006 | −1.53 |
RGS4Cys−* | N/A | N/A |
RGS7 | N/A | N/A |
RGS8 | 11 ± 2 | −0.99 |
RGS16 | 3.5 ± 2.4 | −1.33 |
RGS19 | 0.12 ± 0.02 | −0.61 |
IC50 values in the FCPIA assay show that CCG-50014 is >40 fold more potent for RGS4 than other RGS proteins. Data are presented as: mean IC50 values ± SEM from at least three independent experiments (for RGS4 and RGS8, n >28). N/A: No inhibition below the aqueous solubility limit of the compound (~200 μM).
RGS4Cys− is a mutated form of RGS that contains no cysteine residues in the RGS homology domain (13).