Product Overview
CCG-63808 is a selective inhibitor of RGS4 with IC50 value of 1.4 μM. 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. CCG-63808 is a potent RGS4 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-63808 treatment inhibited GAP activity of RGS4 and the inhibition could be reversed by washing
Synonyms
CCG63808; CCG 63808
Molecular Formula
C25H15FN4O2S
Chemical Name
(E)-2-(1,3-benzothiazol-2-yl)-3-[2-(4-fluorophenoxy)-9-methyl-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request