CCG-50014 is an inhibitor of Regulators of G protein Signaling (RGS) proteins RGS4 and RGS8, which 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 RGS proteins with no affect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.
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