2. Signaling Pathways
  3. GPCR/G Protein
  4. G Protein-coupled Receptor Kinase (GRK)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-123862
    LAS195319
    		Inhibitor
    LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC50 value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and GPCRs. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
    LAS195319
  • HY-150039
    CCG-271423
    		Inhibitor
    CCG-271423 is a potent and selective GRK5 inhibitor with IC50 values of 0.0021 μM and 44 μM for GRK5 and GRK2, respectively. CCG-271423 inhibits cardiomyocyte contractility and decreases in Ca2+ transience. CCG-271423 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CCG-271423
  • HY-118046
    GSK2163632A
    		Inhibitor
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
    GSK2163632A
  • HY-150022
    GRK5-IN-4
    		Inhibitor
    GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research. GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GRK5-IN-4
  • HY-123520
    GSK299115A
    		Inhibitor
    GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor.
    GSK299115A
  • HY-P1396
    GRK2i
    		Inhibitor
    GRK2i is a Gβγ-inhibitory peptide that selectively prevents Gβγ-mediated signaling. GRK2i corresponds to the Gβγ-binding domain of GRK2 (G-protein-coupled receptor kinase 2).
    GRK2i
  • HY-150040
    CCG-273463
    		Inhibitor
    CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 8.6 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer.
    CCG-273463
  • HY-W036034A
    GRK-IN-1
    GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
    GRK-IN-1
  • HY-119232
    GSK466317A
    		Inhibitor
    GSK466317A is a PKA inhibitor, with an IC50 of 12.59 μM. GSK466317A also inhibits GRK1, GRK2, and GRK5, with IC50s of 1000, 31.62, and 39.81 μM, respectively.
    GSK466317A
  • HY-159972
    PKR1 antagonist 1
    		Antagonist
    PKR1 antagonist 1 (PC1) is a potent PKR1 antagonist. PKR1 antagonist 1 reduces hyperalgesia and allodynia in SNI mice.
    PKR1 antagonist 1
  • HY-150021
    GRK5-IN-3
    		Inhibitor
    GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively.
    GRK5-IN-3
  • HY-155099
    FGH31
    		Agonist
    FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin.
    FGH31
  • HY-P990578
    Anti-GPR20 Antibody
    Anti-GPR20 Antibody (DS-6157 antibody) is a human antibody expressed in CHO, targeting GPR20. Anti-GPR20 Antibody has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-GPR20 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-GPR20 Antibody
  • HY-169678
    GRK6-IN-5
    		Inhibitor
    GRK6-IN-5 is a GRK6 polypeptide inhibitor, with IC50 value of 4.48 μΜ. GRK6-IN-5 can be used to study hematological malignancies, inflammation diseases, and autoimmune disorders.
    GRK6-IN-5
  • HY-159996
    GRL093-22
    		Inhibitor
    GRL093-22 is a potent and selective G protein-coupled receptor kinase (GRK) inhibitor, with IC50s of 60 and 40 nM for GRK5 and GRK6, respectively. GRL093-22 has the potential for the research of heart failure and multiple myeloma.
    GRL093-22
  • HY-12976
    DS-1558
    		Agonist
    DS-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.
    DS-1558
  • HY-123254
    CCG-224406
    		Inhibitor
    CCG-224406 is a selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with the IC50 values of 13 nM, greater than 700-fold selectivity over other GRK subfamilies, and no inhibition of ROCK1. CCG-224406 can be used for study of heart failure.
    CCG-224406
Cat. No. Product Name / Synonyms Application Reactivity