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CCG-63802

Cat No.
CEI-1268
Product Overview
CCG-63802 is a selective inhibitor of RGS4 with IC50 value of 1.9 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-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.When tested with HEK-293 cells, administration of CCG-63802 successfully reversed 8-Br-cGMP inhibition on BK via inhibiting RGS4
CAS No.
620112-78-9
Molecular Weight
450.52
Purity
0.98
Storage
Store at -20°C
Synonyms
CCG 63802; CCG63802
Targets
RGS
Molecular Formula
C26H18N4O2S
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
Solubility
Limited solubility
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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