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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.

1 Item

  • BMS-192364
    Cat. No.
    A63814
    CAS No.
    202822-21-7

    BMS-192364

    BMS-192364 is a selective RGS (Regulator of G Protein Signaling) agonist that targets the Gα-RGS interaction, promoting the formation of an inactive Gα-RGS complex. This compound has been shown to reduce urinary bladder contraction and enhance the activity of GTPase-activating proteins (GAPs) on Gq proteins. Additionally, BMS-192364 inhibits calcium flux, making it a valuable tool for studying signaling pathways involved in bladder function and related physiological processes.

    In stock View Details
    5 mg
    $285.00
    10 mg
    $470.00
    All 5 sizes

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