1. Signaling Pathways
  2. GPCR/G Protein
  3. RGS Protein

RGS Protein

Regulators of G-protein Signaling; Regulator of G-protein Signaling

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 (6):

Cat. No. Product Name Effect Purity
  • HY-13509
    Inhibitor 99.42%
    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.
  • HY-U00431
    CCG 203769
    Inhibitor 99.62%
    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.
  • HY-70074
    Inhibitor 99.26%
    CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM.
  • HY-70075
    Inhibitor ≥98.0%
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-114865
    BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux.
  • HY-110054
    CCG-2046 is a RGS4 inhibitor with an IC50 of 4.3 μM against RGS4-Gαo interaction signal.