RGS4 Inhibitor

CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC₅₀ =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.

CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gα_o protein-protein interaction in vitro with an IC₅₀ of 17 nM.

CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gα_o interaction, with an IC₅₀ value of 1.9 μM.

CCG-63808 is a selective, reversible RGS4 inhibitor with an IC₅₀ of 10 μM for the Gα_o-RGS4 interaction. CCG-63808 enhances the contractile response of lymphatic smooth muscle and potentiates agonist-mediated thoracic duct contraction. CCG-63808 can be used in research related to neuropathic pain and hypertension.

CCG-2046 is a RGS4 inhibitor with an IC₅₀ of 4.3 μM against RGS4-Gα_o interaction signal.

CCG-4986 is an RGS protein inhibitor. CCG-4986 inhibits protein activity by covalently modifying the Cys-132 site of RGS4. CCG-4986 can be used to study diseases related to dysregulated G protein-coupled receptor (GPCR) signaling, such as Parkinson's disease and opioid addiction.