1. GPCR/G Protein
  2. RGS Protein

RGS Protein

RGS (Regulators of G protein signaling) are protein structural domains that activate GTPases for heterotrimeric G-protein alpha-subunits. RGS proteins are multi-functional, GTPase-accelerating proteins that promote GTP hydrolysis by the alpha subunit of heterotrimeric G proteins, thereby inactivating the G protein and rapidly switching off G protein-coupled receptor signaling pathways. Upon activation by GPCRs, heterotrimeric G proteins exchange GDP for GTP, are released from the receptor, and dissociate into free, active GTP-bound alpha subunit and beta-gamma dimer, both of which activate downstream effectors. The response is terminated upon GTP hydrolysis by the alpha subunit, which can then bind the beta-gamma dimer and the receptor. RGS proteins markedly reduce the lifespan of GTP-bound alpha subunits by stabilising the G protein transition state. All RGS proteins contain an RGS-box (or RGS domain), which is required for activity. Some small RGS proteins such as RGS1 and RGS4 are little more than an RGS domain, while others also contain additional domains that confer further functionality.

RGS Protein Related Products (3):

Cat. No. Product Name Effect Purity
  • HY-70074
    CCG-63802 Inhibitor
    CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.
  • HY-70075
    CCG-63808 Inhibitor
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-U00431
    CCG 203769 Inhibitor
    CCG-203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.