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CCG215022

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Chemical Structure| 1813527-81-9 同义名 : -
CAS号 : 1813527-81-9
货号 : A152319
分子式 : C26H22FN7O3
纯度 : 98%
分子量 : 499.496
MDL号 : MFCD30489722
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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