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GPCR/G Protein GRK CCG215022

CCG215022

Catalog No. T3498   CAS 1813527-81-9
Purity 99.69% Datasheet

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.

CCG215022, CAS 1813527-81-9
Pack Size Availability Price/USD Quantity
1 mg In stock 141.00
2 mg In stock 225.00
5 mg In stock 400.00
10 mg In stock 580.00
25 mg In stock 1100.00
50 mg In stock 1617.00
100 mg Inquiry 2265.00
1 mL * 10 mM (in DMSO) In stock 400.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.
Targets&IC50 GRK1 :ic50 3.9±1.0μM,   GRK2 :ic50 0.15±0.07μM,   GRK5 :ic50 0.38±0.06μM,   PKA :ic50 120±40μM,  
In vitro CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2[1].
Kinase Assay GRK5 and urea-washed bovine rod outer segments (ROS) are mixed in the dark in buffer containing 20 mM HEPES, pH 7.5, 4 mM MgCl2, and 2 mM EDTA and incubated for 35 min at room temperature. The reaction mixtures are exposed to ambient fluorescent light for 1 min prior to initiation of the reaction by addition of ATP (with [γ-32P]ATP) to a final concentration of 1 mM. Final concentration of GRK5 is 100 nM and ROS is between 0.75 and 24 μM. Reactions are initiated at room temperature, and samples are taken at 2-5 min and then quenched with SDS-PAGE loading dye. Proteins are separated using SDS-PAGE, gel is dried, and the incorporation of γ-32P is detected using a phosphor storage screen. Rates at 0 min are plotted against the ROS concentration, and Vmax and Kmvalues are determined using the Michaelis-Menten equation. Vmax of each curve is normalized to the Vmax of GRK5561 run in parallel. Melting point determinations in response to 200 μM CCG215022 are performed in 20 mM HEPES, pH 7.0, 5 mM MgCl2, 2 mM DTT, 1 mM CHAPS at a final GRK5 concentration of 0.2 mg/mL and 100 μM anilinonaphthalene-8-sulfonic acid using a ThermoFluor plate reader. Melting points of GRK5 variants are assayed in a buffer containing 20 mM HEPES, pH 8.0, 200 mM NaCl, 2 mM DTT, 2.5 mM MgCl2, and 0.1 mM anilinonaphthalene-8-sulfonic acid with or without 5 mM ATP. Final GRK5 concentration for these assays is 0.1 mg/mL[1].
Appearance solid
Molecular Weight 499.51
Formula C26H22FN7O3
CAS No. 1813527-81-9

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 28 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Homan KT, et al. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally DesignedInhibitor. J Biol Chem. 2015 Aug 21;290(34):20649-59.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Kinase Inhibitor Library GPCR Compound Library Fluorochemical Library

Related Products

Related compounds with same targets
Paroxetine hydrochloride CCG215022 GSK180736A Ellagic acid Piceatannol Bucladesine sodium salt BX912 Theophylline-7-acetic acid

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