CCG-63802

Short Summary : RGS protein inhibitor

Category : GPCR/G protein|RGS

Purity : 0.98

CAS Number : 620112-78-9

Formula : C26H18N4O2S

Molecular Weight : 450.52

SMILE : CC1=CC(=CC=C1)OC2=C(C(=O)N3C=CC=C(C3=N2)C)C=C(C#N)C4=NC5=CC=CC=C5S4

Solubility : Limited solubility

Storage : Store at -20°C

Description : CCG-63802 is a selective inhibitor of RGS4 with IC50 value of 1.9 μM [1].RGS (regulators of G protein signaling) are multi-functional, GTPase-accelerating proteins and plays an important role in promoting GTP hydrolysis via heterotrimeric G proteins α subunit. RGS 4 is also known as RGP4 and plays a pivotal role in negatively regulating signaling upstream or at the level of the heterotrimeric G protein [1, 2].CCG-63802 is a potent RGS inhibitor and is different from the reported RGS4 irreversibly inhibitor CCG-4986. Using the [32P] GTP single-turnover GAP assay, it was shown that CCG-63802 treatment inhibited GAP activity of RGS4 [1]. When tested with HEK-293 cells, administration of CCG-63802 successfully reversed 8-Br-cGMP inhibition on BK via inhibiting RGS4 [2].References: [1].Blazer, L.L., et al., Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol, 2010. 78(3): p. 524-33.[2].Dobrivojevic, M., et al., Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol, 2012. 303(12): p. C1260-8.

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