CCG-63802

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CCG-63802 是 G 蛋白信号传导 (RGS) 蛋白调节因子的可逆小分子抑制剂。

CCG-63802 is a reversible small-molecule inhibitor of regulator of G protein signaling (RGS) proteins. CCG-63802 inhibits the interaction between RGS4 and Galpha with an IC50 value of 1.4 μM.(In Vitro):CCG-63802 showed selectivity among RGS proteins with a potency order of RGS 4 > 19 = 16 > 8 ? 7. CCG-63802 inhibited the GTPase accelerating protein activity of RGS4.(In Vivo):The attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling was partially abrogated by administration of RGS4 inhibitor CCG-63802(0.5 mg/kg). The downregulation of RGS4 by CCG-63802 also significantly increased inflammatory cell accumulation and AHR, and increased levels of IL-4, IL-13, eotaxin, IFN-γ, and IL-17A in BALF, and total and OV-specific IgE in serum. The inhibitory effects of PGZ on the activations of ERK and Akt/mTOR signaling, and MMPs were apparently reversed by CCG-63802 administration.

CCG-63802 (5 μM) inhibits regulators of G-protein signaling (RGS) proteins in the presence of BK (bradykinin) and 8-Br-cGMP (membrane-permeable analogue of cGMP), HEK-293 cells start to depolarize again.

CCG-63802 (0.05 mg/kg; intratracheal administration; once per week; 90 days) reduces RGS4 protein expression, leading to partially abrogate the attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling. Animal Model:Forty female BALB/c mice aged 6-8 week oldDosage:0.05 mg/kg Administration:Intratracheal administration; once per week; 90 days Result:CCG 63802 treatment in OVA +PGZ + CCG group significantly reduced RGS4 protein expression compared to OVA + PGZ group (P < 0.05)

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Others

Other Targets

Microtubule/Tubulin

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620112-78-9

450.52

C26H18N4O2S

>98% (HPLC)

In Vitro:?DMSO : 1.67 mg/mL (3.71 mM)

Cc1cccc(Oc2nc3c(C)cccn3c(=O)c2\C=C(/C#N)c2nc3ccccc3s2)c1

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(-20℃)

With Ice Pack

≥ 2 years