G Protein-coupled Receptor Kinase (GRK)
G protein-coupled receptor kinases (GRKs) are a family of serine/threonine kinases that phosphorylate agonist-bound, or activated, G protein-coupled receptors (GPCRs) as their primary substrates. On the basis of their sequence homology, GRKs can be subclassified into three groups: the visual subfamily (GRK1 and GRK7), the GRK4 subfamily (GRK4, GRK5 and GRK6) and the β-AR kinase (βARK) subfamily (GRK2 and GRK3). GRK1 and GRK7 are primarily expressed in retinal photoreceptor cells, whereas GRK4 is most abundantly expressed in the testes. GRK2, GRK3 and GRK5 are ubiquitously expressed, albeit to various extents in different tissues. In the heart, GRK2 and GRK5 are most prominent, whereas GRK3 and GRK6 are expressed at low levels. Functionally, all GRKs mediate the uncoupling and internalization of activated GPCRs. All GRKs are primarily localized to the cytosol and plasma membrane. GRK1, GRK4, GRK5, GRK6 and GRK7 are basally localized to the membrane. Conversely, GRK2 and GRK3 are primarily localized to the cytosol and translocate to the membrane after receptor stimulation.
All Product Categories
-
G Protein-coupled Receptor Kinase (GRK) Inhibitors
(46)
View all products
-
G Protein-coupled Receptor Kinase (GRK) Agonists
(2)
View all products
-
G Protein-coupled Receptor Kinase (GRK) Modulators
(3)
View all products
-
G Protein-coupled Receptor Kinase (GRK) Degrader
(1)
View all products
-
G Protein-coupled Receptor Kinase (GRK) Substrate
(1)
View all products
-
G Protein-coupled Receptor Kinase (GRK) Related Products (64)
Related Products (64)
-
Antibodies (2)
-
CMPD101 (Standard)
0 ImagesCat. No.: HY-103045RCAS No.: 865608-11-3CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
-
Grk2 Mouse Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS16845Grk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Grk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
-
GRK5-IN-5
0 ImagesCat. No.: HY-180583CAS No.: 3061801-11-1GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy.
-
DS-1558
0 ImagesCat. No.: HY-12976CAS No.: 1202575-67-4DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes.
