620112-78-9

620112-78-9 structure

Name: CCG-63802
Chemical Name: (E)-2-(1,3-benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile
CAS Number: 620112-78-9
Molecular Formula: C₂₆H₁₈N₄O₂S
Molecular Weight: 450.51200
Catalog: Signaling Pathways GPCR/G Protein RGS Protein
Create Date: 2018-12-30 15:50:14
Modify Date: 2024-01-10 08:51:34
CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.IC50 value:Target: RGSCCG-63802 is selective amongst RGS proteins, with greatest potency at RGS4. CCG-63802 inhibits GTPase accelerating protein activity of RGS4 and blocks its interaction with Gαo. Retains activity under reducing conditions.

Name	(E)-2-(1,3-benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile
Synonyms	unii-339bu4y35u hms1804i11 CCG-63802

Description	CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.IC50 value:Target: RGSCCG-63802 is selective amongst RGS proteins, with greatest potency at RGS4. CCG-63802 inhibits GTPase accelerating protein activity of RGS4 and blocks its interaction with Gαo. Retains activity under reducing conditions.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> RGS Protein Research Areas >> Cancer
References	[1]. Blazer LL, et al. Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol. 2010 Sep;78(3):524-33. [2]. Bosier B, et al. Inhibition of the regulator of G protein signalling RGS4 in the spinal cord decreases neuropathic hyperalgesia and restores cannabinoid CB1 receptor signalling. Br J Pharmacol. 2015 Nov;172(22):5333-46. [3]. Meng X, et al. PPARγ Agonist PGZ Attenuates OVA-Induced Airway Inflammation and Airway Remodeling via RGS4 Signaling in Mouse Model. Inflammation. 2018 Jul 19.