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CCG215022 {[allProObj[0].p_purity_real_show]}

货号:A152319

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.

CCG215022 化学结构 CAS号:1813527-81-9
CCG215022 化学结构
CAS号:1813527-81-9
CCG215022 3D分子结构
CAS号:1813527-81-9
CCG215022 化学结构 CAS号:1813527-81-9
CCG215022 3D分子结构 CAS号:1813527-81-9
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CCG215022 纯度/质量文件 产品仅供科研

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CCG215022 生物活性

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].

CCG215022 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

CCG215022 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

10.01mL

2.00mL

1.00mL

20.02mL

4.00mL

2.00mL

CCG215022 技术信息

CAS号1813527-81-9
分子式C26H22FN7O3
分子量 499.496
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 30 mg/mL(60.06 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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