CCG 50014 CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM. In vitro
CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys−). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4−Gαo protein−protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment. [1] [2]
