同义名 :	-
	CAS号 :	1813527-81-9
	货号 :	A152319
	分子式 :	C26H22FN7O3
	纯度 :	99%
	分子量 :	499.5
	MDL号 :	MFCD30489722
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	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