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-149720
    GRL018-21
    		Inhibitor
    GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 value of 10 nM.
    GRL018-21
  • HY-129118
    Takeda103A
    		Inhibitor 98.69%
    Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure.
    Takeda103A
  • HY-P0204
    Endothelin-3, human, mouse, rabbit, rat
    Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
    Endothelin-3, human, mouse, rabbit, rat
  • HY-109562
    CCG258208
    		Inhibitor
    CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research.
    CCG258208
  • HY-128311
    GRK6-IN-3
    		Inhibitor
    GRK6-IN-3 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 1.03 μM.
    GRK6-IN-3
  • HY-B0492R
    Paroxetine hydrochloride (Standard)
    		Inhibitor
    Paroxetine (hydrochloride) (Standard) is the analytical standard of Paroxetine (hydrochloride). This product is intended for research and analytical applications. Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
    Paroxetine hydrochloride (Standard)
  • HY-B0492AR
    Paroxetine hydrochloride hemihydrate (Standard)
    		Inhibitor
    Paroxetine (hydrochloride hemihydrate) (Standard) is the analytical standard of Paroxetine (hydrochloride hemihydrate). This product is intended for research and analytical applications. Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14?μM.
    Paroxetine hydrochloride hemihydrate (Standard)
  • HY-P3035
    Corazonin
    Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species.
    Corazonin
  • HY-111239
    GSK317354A
    		Inhibitor
    GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.
    GSK317354A
  • 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-W783254
    C18 LPA
    C18 LPA (PA(18:0e/0:0)) is a water-soluble phospholipid that functions as a signaling molecule, influencing various cellular responses through G protein-coupled receptors (GPCRs). It is known to promote smooth muscle contraction, cytoskeletal rearrangement, and chemotaxis, while also playing a role in neurotransmitter release, cell proliferation, platelet aggregation, and Ca2+ mobilization. Elevated levels of C18 LPA in human plasma are associated with ovarian cancer and atherosclerosis, suggesting its potential as a biomarker for ovarian cancer.
    C18 LPA
  • HY-W036034A
    GRK-IN-1
    GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
    GRK-IN-1
  • 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
  • HY-RS05813
    GRK2 Human Pre-designed siRNA Set A
    		Inhibitor

    GRK2 Human Pre-designed siRNA Set A contains three designed siRNAs for GRK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    GRK2 Human Pre-designed siRNA Set A
    GRK2 Human Pre-designed siRNA Set A
Cat. No. Product Name / Synonyms Application Reactivity