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CCG215022

カタログ番号GC19090

CCG215022は、GRK2、GRK5およびGRK1に対してそれぞれ0.15±0.07μM、0.38±0.06μMおよび3.9±1μMのIC50を有するGタンパク質共役受容体キナーゼ(GRK)阻害剤である。

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CCG215022 化学構造

Cas No.: 1813527-81-9

サイズ 価格 在庫数 個数
1mg
$94.00
在庫あり
5mg
$235.00
在庫あり
10mg
$335.00
在庫あり
50mg
$1,004.00
在庫あり
100mg
$1,406.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

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].

References:

[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.

Background

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.

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].

References:
[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.

Chemical Properties

Cas No. 1813527-81-9 SDF
Canonical SMILES CC(N1)=C(C(NC2=CC=C(NN=C3)C3=C2)=O)C(C4=CC(C(NCC5=CC=CC=N5)=O)=C(F)C=C4)NC1=O
Formula C26H22FN7O3 M.Wt 499.5
溶解度 DMSO : ≥ 28 mg/mL (56.06 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.002 mL 10.01 mL 20.02 mL
5 mM 0.4004 mL 2.002 mL 4.004 mL
10 mM 0.2002 mL 1.001 mL 2.002 mL
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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