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CCG-63802

Catalog No.
A3289
RGS protein inhibitor
Grouped product items
SizePriceStock Qty
5mg
$86.00
Ship with 10-15 days
10mg
$144.00
Ship with 10-15 days
50mg
$459.00
Ship with 10-15 days
100mg
$737.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceYellow solid
StorageStore at -20°C
M.Wt450.52
Cas No.620112-78-9
FormulaC26H18N4O2S
SynonymsCCG 63802;CCG63802
SolubilityLimited solubility, soluble in DMSO
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
SDFDownload SDF
Canonical SMILESCC1=CC(=CC=C1)OC2=C(C(=O)N3C=CC=C(C3=N2)C)C=C(C#N)C4=NC5=CC=CC=C5S4
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

CCG-63802