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-B0492
    Paroxetine hydrochloride
    		Inhibitor 99.96%
    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
  • HY-103045
    CMPD101
    		Inhibitor 98.95%
    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.
    CMPD101
  • HY-142812
    GRK6-IN-1
    		99.61%
    GRK6-IN-1 (Compound 18) is the inhibitor for G protein-coupled receptorkinase 6 (GRK6) with an IC50 of 3.8-8 nM. GRK6-IN-1 also inhibits GRK7, GRK5, GRK4 and GRK1 with IC50s of 6.4, 12, 22 and 52 nM, respectively. GRK6-IN-1 has the potential for the research of multiple myeloma.
    GRK6-IN-1
  • HY-121983
    CAY10594
    		Modulator 98.64%
    CAY10594 is an orally active PLD2 inhibitor with an IC50 of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.
    CAY10594
  • HY-136561
    GRK5-IN-2
    		99.92%
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 of 49.7 μM. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
    GRK5-IN-2
  • HY-128231
    GRK6-IN-4
    		Inhibitor
    GRK6-IN-4 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 of 1.56 μM. GRK6-IN-4 can be utilized in research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.
    GRK6-IN-4
  • HY-168971
    Paeoniflorin-6′-O-benzene sulfonate
    		Inhibitor
    Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model.
    Paeoniflorin-6′-O-benzene sulfonate
  • 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-W013411A
    Locostatin
    		Inhibitor 99.88%
    Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
    Locostatin
  • HY-109562A
    CCG258208 hydrochloride
    		98.05%
    CCG258208 (GRK2-IN-1) hydrochloride 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 hydrochloride can be used in heart failure research.
    CCG258208 hydrochloride
  • HY-142817
    GRK6-IN-2
    		98.98%
    GRK6-IN-2 (compound 10a) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for the research of multiple myeloma.
    GRK6-IN-2
  • HY-18991
    CCG215022
    		Inhibitor 99.79%
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
    CCG215022
  • HY-156863
    GRK2 Inhibitor 2
    		Inhibitor 98.88%
    GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC50 of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC50 of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF).
    GRK2 Inhibitor 2
  • HY-18990
    GSK180736A
    		Inhibitor 98.81%
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
    GSK180736A
  • HY-143248
    KR-39038
    		Inhibitor 99.48%
    KR-39038 is an orally active and potent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 0.02 μM. KR-39038 significantly inhibits angiotensin II-induced cellular hypertrophy through suppression of HDAC5 pathway in neonatal cardiomyocytes. KR-39038 shows profound anti-hypertrophic effects and improved cardiac function. KR-39038 can be used for heart failure research.
    KR-39038
  • HY-47573
    CCG273441
    		Inhibitor 98.78%
    CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle.
    CCG273441
  • HY-123538
    GRK2 Inhibitor 1
    		Inhibitor 98.06%
    GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time.
    GRK2 Inhibitor 1
  • HY-B0492A
    Paroxetine hydrochloride hemihydrate
    		Inhibitor 99.96%
    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
  • HY-139690
    CCG258747
    		Inhibitor 98.96%
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
    CCG258747
  • HY-P1396A
    GRK2i TFA
    		Inhibitor 98.41%
    GRK2i TFA is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. GRK2i TFA corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist.
    GRK2i TFA
Cat. No. Product Name / Synonyms Application Reactivity