CCG 203769 是一种选择性的 RGS4 抑制剂，对 RGS4-Gαo 蛋白-蛋白相互作用的 IC50 为 17 nM。

CCG 203769 is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.

CCG 203769 displays dramatic selectivity (8- to >5000-fold) for RGS4 over other RGS proteins with IC50s of 140 nM, 6 μM, and 79 μM for RGS19, RGS16, and RGS8. CCG 203769 inhibits GSK-3β with an IC50 of 5 μM. CCG 203769 enhances Gαq-dependent cellular Ca2+ signaling in an RGS4-dependent manner and inhibits RGS/Gαo binding in an RGS-selective manner. CCG 203769 also blocks the GTPase accelerating protein (GAP) activity of RGS4. CCG 203769 inhibits the effect of GTP hydrolysis stimulated by RGS4 with an IC50<1 μM in single-turnover and steady-state GTPase experiments[1].

CCG 203769 (10 mg/kg, i.v.), administered immediately prior to Carbamoylcholine chloride(0.1 mg/kg, i.p.), significantly potentiates the bradycardic effect. CCG 203769 (1-10 mg/kg) reverses the increased hang time caused by raclopride administration in rats. CCG 203769 (0.1-10 mg/kg) reverses the raclopride-induced paw drag in mice[1].

410074-60-1

C8H14N2O2S

202.27

Thiadiazolidinone (TDZD) deriv. 6;4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione;RGS4 inhibitor 11b

DMSO:50 mg/mL (247.2 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years