CCG-4986 is the first selective non-peptide inhibitor of the regulator of G protein signaling protein subtype RGS4.1 It covalently2-3 modifies RGS4 by inhibiting its interaction with Galpha (IC50 = 3-5 mM) and suppressing GTPase activity1. Intratympanic administration of CCG-4986 was shown to rescue cochlear injury and hearing loss induced by acoustic overexposure and represents a novel paradigm for the treatment of sensorineural hearing loss via pharmacological regulation of GPCR signaling.4 A novel tool for exploring the involvement of RGS4 in physiological processes.5
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