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CAS No.: 1813527-81-9

CCG215022 Catalog No. CSN19161

Synonyms: CCG-215022

CCG-215022 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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 GRK2

IC50:0.15±0.07μM GRK5

IC50:0.38±0.06μM GRK1

IC50:3.9±1μM
描述G protein-coupled receptor kinases (GRKs) regulate cell signaling by initiating the desensitization of active G protein-coupled receptors. CCG-215022 is a potently GRKs inhibitor with IC50 values of 3.9nM, 0.15nM, 0.38nM and 120nM for GRK1, GRK2, GRK5 and PKA, respectively^[1]. Treatment of murine cardiomyocytes with 0.5μM CCG215022 resulted in significantly increased contractility at 20-fold lower concentrations than paroxetine, an inhibitor with more modest selectivity for GRK2^[1]. CCG-215022 also inhibited the desensitization of H1 or P2Y2 receptor driven PLC/Ca²⁺ activity in ULTR and MSMC with IC50 values of 5.51μM and 5.53μM, respectively^[2]. In vivo, intraperitoneal administration CCG-215022 at 20mg/kg every 3 days for 21 days significantly reduce tumor growth in ERMS and ARMS xenograft tumor models^[3].
作用机制The amide-linked pyridine extension of CCG215022 forms additional hydrogen bonds via its amide with the P-loop and via the pyridine nitrogen with Lys220 and Asp329 ^[4].
参考文献

[1] Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor. Journal of Biological Chemistry, 2015, 290(34): 20649-20659
[2] Rainbow R D, Brennan S, Jackson R, et al. Small-Molecule G Protein-Coupled Receptor Kinase Inhibitors Attenuate G Protein-Coupled Receptor Kinase 2-Mediated Desensitization of Vasoconstrictor-Induced Arterial Contractions. Molecular Pharmacology, 2018, 94(3): 1079-1091
[3] Pham T Q, Robinson K, Vleeshouwerneumann T, et al. Characterization of GRK5 as a novel regulator of rhabdomyosarcoma tumor cell growth and self-renewal. bioRxiv, 2019
[4] Waldschmidt H V, Bouley R, Kirchhoff P D, et al. Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors. Bioorganic & Medicinal Chemistry Letters, 2018, 28(9): 1507-1515

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0020 mL
- 10.0101 mL
- 20.0202 mL
- 5 mM
- 0.4004 mL
- 2.0020 mL
- 4.0040 mL
- 10 mM
- 0.2002 mL
- 1.0010 mL
- 2.0020 mL

技术信息

CAS号

1813527-81-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H22FN7O3

运输

蓝冰

分子量

499.50

别名

CCG-215022

溶解度

DMSO	100.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	Insoluble

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靶点	Description	IC50
GRK2		IC50:0.15±0.07μM
GRK5		IC50:0.38±0.06μM
GRK1		IC50:3.9±1μM

CCG215022 Catalog No. CSN19161

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