Regulators of G-protein signaling (RGS) proteins are potent negative modulators of signal transduction through G-protein-coupled receptors. CCG-50014 is the most potent small molecule RGS inhibitor to date, with broad application prospects in both therapeutic and research fields. Researches show that CCG-50014 fully inhibits several RGS proteins, including RGS8, RGS16, and RGS19, and is highly potent at inhibiting RGS4. However, it did not have activity on RGS7.
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