1. Signaling Pathways
  2. GPCR/G Protein
  3. 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 相关产品 (4):

Cat. No. Product Name Effect Purity
  • HY-U00431
    CCG 203769 Inhibitor 99.93%
    CCG 203769 是一种选择性的 G 蛋白信号调节因子 (RGS4) 抑制剂,CCG 203769 阻断 RGS4-Gαo 蛋白-蛋白相互作用,IC50 为 17 nM。
  • HY-70074
    CCG-63802 Inhibitor 98.38%
    CCG-63802是可逆的G蛋白信号调节子(RGS)抑制剂,对RGS4抑制性尤其高。
  • HY-70075
    CCG-63808 Inhibitor
    CCG-63808 是可逆的G蛋白信号调节子(RGS)抑制剂。
  • HY-13509
    CCG-50014 Inhibitor >99.0%
    CCG-50014 是 RGS4 抑制剂 (IC50=30 nM),对 RGS4 的选择性比其他 RGS 蛋白高 20 倍。CCG-50014 与 RGS 共价结合,在位于变构调节位点的两个半胱氨酸残基上形成加合物。CCG50014 在小鼠福尔马林试验中减少伤害性反应并增强阿片类药物介导的镇痛作用。
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