L 2-401

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. RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins. CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα₀, while blocking GTPase activity and Gα₀-dependent translocation of RGS4 to the membrane.