2. Signaling Pathways
  3. GPCR/G Protein
  4. RGS Protein
  5. RGS16 Isoform

RGS16

RGS16 (Regulator of G-protein Signaling 16) is a member of the R4 subfamily of RGS proteins that accelerates GTP hydrolysis on Gα subunits and thereby terminates or constrains GPCR signaling outputs[1][2]. Mechanistically, RGS16 regulates classical GPCR pathways and also influences downstream signaling networks including MAPK, PI3K/Akt, RhoA, and SDF-1/CXCR4 pathways, linking receptor activation to immune, inflammatory, metabolic, and tumor-associated biological processes[1]. In metabolic models, hepatic RGS16 expression is induced during gluconeogenic states and provides a mechanism through which glucose production suppresses GPCR-stimulated fatty-acid oxidation, highlighting a role in energy homeostasis[3]. In pancreatic islets, RGS16 functions as a regulator of β-cell physiology by attenuating inhibitory Gαi/o-dependent somatostatin signaling, thereby promoting cAMP accumulation, insulin secretion, and β-cell proliferation in both rodent and human systems[4]. RGS16 also contributes to circadian regulation, where it is required for cAMP control within the suprachiasmatic nucleus and is linked to GPCR-mediated clock signaling mechanisms[5]. Compared with related RGS isoforms, RGS16 belongs to the small R4 family but displays distinct G-protein selectivity and signaling interactions that contribute to nonredundant biological functions across tissues[2]. For experimental applications, modulation of RGS proteins is widely explored as a strategy to control GPCR signal transduction, making RGS16 a useful target for mechanistic studies of metabolism, immunity, circadian biology, and disease-associated signaling networks[1][6].

RGS16 Related Products (2):

Cat. No. Product Name Effect Purity
  • HY-13509
    CCG-50014
    		Inhibitor 99.62%
    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 99.76%
    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.