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

RGS Protein (RGS蛋白)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13509
    CCG-50014 Inhibitor 99.42%
    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活性分子介导减缓疼痛的作用。
    CCG-50014
  • HY-U00431
    CCG 203769 Inhibitor 99.76%
    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。
    CCG 203769
  • HY-70074
    CCG-63802 Inhibitor 99.26%
    CCG-63802 是一种选择性,可逆变构的 G 蛋白信号调节子 RGS4 抑制剂。CCG-63802 与 RGS4 特异性结合并阻断 RGS4-Gαo 相互作用,IC50 值为 1.9 μM。
    CCG-63802
  • HY-114865
    BMS-192364 Agonist 99.01%
    BMS-192364 靶向 Gα-RGS 相互作用以产生无活性的 Gα-RGS 复合物。BMS-192364 通过增加 GAP 对 Gq 蛋白的作用来减少膀胱收缩并发挥 RGS 激动剂特性。BMS-192364 抑制钙通量。
    BMS-192364
  • HY-70075
    CCG-63808 Inhibitor ≥98.0%
    CCG-63808 是可逆的G蛋白信号调节子(RGS)抑制剂。
    CCG-63808
  • HY-122251
    CCG-4986 Inhibitor
    CCG-4986 是一种 RGS protein 抑制剂。CCG-4986 通过对 RGS4 的 Cys-132 位点进行共价修饰来抑制蛋白活性。CCG-4986 可用于 G 蛋白偶联受体 (GPCR) 信号失调的相关疾病研究,如帕金森氏病和阿片类药物成瘾。
    CCG-4986
  • HY-110054
    CCG-2046 Inhibitor
    CCG-2046 是一种 RGS4 抑制剂,对 RGS4-Gαo 交流信号的 IC50 为 4.3 μM。
    CCG-2046
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