CCG-50014 (CCG50014) is a potent, selective, covalent inhibitor of RGS4 with IC50 of 30 nM; dispalys >20-fold selective for RGS4 over other RGS proteins; binds in an allosteric regulatory site, does not inhibit activity of the cysteine protease papain; reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test; a useful tool for studying the functional roles of RGS4.
