CCG-63802 may be used to study G-protein-mediated cell signaling.
CCG-63802 is a selective, reversible inhibitor of the G protein signaling regulator RGS4. It specifically binds to RGS4 and blocks RGS4-Gαo interaction with IC50 value of 1.9 μM.
CCG-63802 (5 μM) inhibits regulators of G-protein signaling (RGS) proteins in the presence of BK (bradykinin) and 8-Br-cGMP (membrane-permeable analogue of cGMP), HEK-293 cells start to depolarize again.
CCG-63802 (0.05 mg/kg; intratracheal administration; once per week; 90 days) reduces RGS4 protein expression, leading to partially abrogate the attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling .