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Beschreibung

A cell-permeable, thiadiazolidinone based, thiol reactive compound that covalently binds to the regulator of G protein signaling 4 (RGS4) and irreversibly inhibits its activity (IC50 = 17 nM). Exhibits high selectivity over RGS19 and RGS16 (IC50 = 140 nM and 6 µ,M, respectively) and has negligible effects towards RGS7, RGS8, and papain IC50 = 100, 70, and 100 µ,M, respectively). Displays ~300-fold greater selectivity over GSK-3beta (IC50 = 5.4 µ,M). Shown to disrupt RGS4/Galphao interaction and reverse the Galphao-induced membrane translocation of GFP-tagged RGS4 in HEK293 cells (~3 µ,M). Enhances Galphaq-dependent Ca2+ signaling activated by the M3 muscarinic receptor. Potentiates Galphai-dependent muscarinic bradycardia and reverses D2 antagonist raclopride-induced akinesia and bradykinesia in a murine model of the movement disorder in Parkinson's disease.