CCG-50014
CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins.{19235} RGS proteins bind to the G? subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins.{19235} CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on G?0, while blocking GTPase activity and G?0-dependent translocation of RGS4 to the membrane.{19235}
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