For research use only. Not for therapeutic Use.
CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM[1].
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[2].
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[3].
| Catalog Number | I004340 |
| CAS Number | 620112-78-9 |
| Synonyms | (E)-2-(1,3-benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile |
| Molecular Formula | C26H18N4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C26H18N4O2S/c1-16-7-5-9-19(13-16)32-24-20(26(31)30-12-6-8-17(2)23(30)29-24)14-18(15-27)25-28-21-10-3-4-11-22(21)33-25/h3-14H,1-2H3/b18-14+ |
| InChIKey | VFSVKVQMZDJFQX-NBVRZTHBSA-N |
| SMILES | CC1=CC(=CC=C1)OC2=C(C(=O)N3C=CC=C(C3=N2)C)C=C(C#N)C4=NC5=CC=CC=C5S4 |
| Reference | [1]. Levi L Blazer, et al. Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol. 2010 Sep;78(3):524-33. [2]. Marina Dobrivojević, et al. Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1260-8. [3]. Xia Meng, et al. PPARγ Agonist PGZ Attenuates OVA-Induced Airway Inflammation and Airway Remodeling via RGS4 Signaling in Mouse Model. Inflammation. 2018 Dec;41(6):2079-2089. |
