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RGS Protein

RGS protein inhibitors act on regulators of G protein signaling that switch off active Gα subunits. Regulator of G protein signaling (RGS) proteins share a conserved RGS domain that binds the GTP-bound Gα subunit. In 1996, RGS4 and the Gα-interacting protein (GAIP) were shown to be GTPase-activating proteins for the Gi subfamily of Gα subunits. By speeding GTP hydrolysis, RGS proteins shorten the signals sent by many G protein-coupled receptors (GPCRs). CCG-4986 came from a 2007 flow cytometry screen for compounds that disrupt binding between RGS4 and Gα. CCG-63802 and CCG-63808, described in 2010, are reversible inhibitors that act at an allosteric site. CCG 50014 is listed as an RGS4 inhibitor, and the set also includes RGS10 and RGS14 modulators.

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  • RGS10 modulator-1
    Cat. No.
    A63815
    CAS No.
    1113116-62-3

    RGS10 modulator-1

    RGS10 modulator-1 functions as a potent modulator of the RGS10 protein, exhibiting significant biological activity by reversing interferon-gamma (IFNγ)-induced expression of RGS10 protein and mRNA. Additionally, this compound effectively reduces the levels of COX-2 mRNA and inducible nitric oxide synthase (iNOS) expression that are stimulated by IFNγ. RGS10 modulator-1 is a valuable tool for research exploring the regulatory mechanisms of RGS10 in inflammatory responses and related signaling pathways.

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