GRK

G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases within the AGC (protein kinase A, protein kinase G, protein kinase C) group of kinases. Like all AGC kinases, GRKs use ATP to add phosphate to Serine and Threonine residues in specific locations of target proteins. In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways.

Cat. No.	Product Name	CAS No.	Purity
T1636	Paroxetine hydrochloride 盐酸帕罗西汀	78246-49-8	99.91%
T1636	Paroxetine hydrochloride 是一种血清素摄取抑制剂，能抑制 GRK2 活性，IC50值为 14 μM。它可研究抑郁症。
T8913	1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID 化合物T8913	260555-42-8	99.78%
T8913	1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID 靶向 GRK2。
T14989	CMPD101 化合物CMPD101	865608-11-3	99.01%
T14989	CMPD101 是膜透性的GRK2/3高选择性小分子抑制剂，IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小，IC50值分别为 3.1 μM，2.3 μM，1.4 μM 和 8.1 μM，可研究心衰疾病。
T3513	GSK180736A 化合物GSK180736A	817194-38-0	98.44%
T3513	GSK180736A 是 Rho 相关卷曲螺旋激酶 1 (ROCK1) 抑制剂，IC50值为 100 nM。它也是选择性的ATP-竞争性 G 蛋白偶联受体激酶 2 抑制剂，IC50值为 0.77 μM，其选择性比其他 GRK 高 100 倍以上。
T24850	Takeda103A 化合物Takeda103A	865609-72-9	98.01%
T24850	Takeda103A 是GRK2抑制剂。G 蛋白偶联受体是许多生理过程的核心。Takeda103A 对研究心力衰竭具有潜在的研究价值。
T3498	CCG215022 化合物CCG215022	1813527-81-9	98%
T3498	CCG215022 是G蛋白偶联受体激酶抑制剂，能够作用于GRK2 (IC50:0.15±0.07 μM)，GRK5 (IC50:0.38±0.06 μM) 和 GRK1 (IC50:3.9±1 μM)。
T9609	GRK5-IN-2 化合物GRK5-IN-2	1642839-27-7	98%
T9609	GRK5-IN-2 是基于吡啶的双环化合物，抑制G 蛋白偶联受体激酶 5 。它调节胰岛素的表达和/或释放，在代谢疾病中有研究价值。
T27467	GSK270822A 化合物GSK270822A	864082-23-5	98%
T27467	GSK270822A是一种选择性的ROCK1抑制剂。GSK270822A抑制ROCK1，RSK1，p70S6K的IC50 分别为9nM，1100nM，1550nM。
T27471	GSK299115A 化合物GSK299115A	864082-35-9	98%
T27471	GSK299115A是一种选择性的ROCK1抑制剂。GSK299115A抑制ROCK1、RSK1和p70S6K的IC50分别为8nM、620nM和560nM。
T13714L	GRK2-IN-1 hydrochloride (2055990-90-2 free base) 化合物 T13714L	T13714L	98%
T13714L	GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
T13714	CCG258208 化合物 T13714	2055990-90-2	98%
T13714	GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).