CCG 50014 是一种有效的选择性 RGS4 抑制剂，IC50 为 30 nM。它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减缓疼痛的作用。它与 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。

CCG 50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.

CCG-50014 is highly potent at inhibiting RGS4 and it fully inhibits several other RGS proteins, including RGS8, -16, and -19, but does not have activity on RGS7. Furthermore, CCG-50014 has no activity on a mutated form of RGS4 that lacks cysteine residues in the RGS homology domain (RGS4Cys?). CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG-50014 is able to inhibit the RGS4?Gαo protein?protein interaction in a living cell. CCG-50014 represents the first of a class of small molecule RGS inhibitors that function in a cellular environment. [1] [2]

883050-24-6

C16H13FN2O2S

316.35

CCG 50014;4-[(4-氟苯基)甲基]-2-(4-甲基苯基)-1,2,4-噻二唑烷-3,5-二酮

DMSO:59 mg/mL (186.5 mM)
Ethanol:<1 mgml
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years