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.
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G Protein-coupled Receptor Kinase (GRK) Inhibitors
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G Protein-coupled Receptor Kinase (GRK) Agonists
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G Protein-coupled Receptor Kinase (GRK) Modulators
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G Protein-coupled Receptor Kinase (GRK) Degrader
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G Protein-coupled Receptor Kinase (GRK) Substrate
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G Protein-coupled Receptor Kinase (GRK) Related Products (66)
Related Products (66)
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Antibodies (2)
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GSK2163632A
0 ImagesCat. No.: HY-118046CAS No.: 1123163-20-1GSK2163632A 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).
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GRK5-IN-4
0 ImagesCat. No.: HY-150022CAS No.: 2410794-89-5Synonyms: CCG-265328GRK5-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.
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GRK6-IN-4
0 ImagesCat. No.: HY-128231CAS No.: 300731-73-1GRK6-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.
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CCG 258001
0 ImagesCat. No.: HY-120168CAS No.: 2055990-96-8CCG 258001 is a GRK inhibitor with IC50 values of 0.29, 51.8, and 33 µM against GRK2, GRK1, and GRK5, respectively. CCG 258001 inhibits GRK activity in cardiomyocytes and other muscle cells. CCG 258001 is applicable to the research of heart diseases, including heart failure, myocardial hypertrophy, and hypertension.
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GRK2 modulator 1
0 ImagesCat. No.: HY-183057CAS No.: 2234900-83-3GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD.
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Obuprazine
0 ImagesCat. No.: HY-183734CAS No.: 2640663-79-0Obuprazine is an orally active dopamine D3 receptor agonist and 5-HT2A receptor antagonist with IC50 values of 0.37 and 4.19 nM, respectively. Obuprazine acts as a G protein-coupled receptor modulater. Obuprazine can be used for the research of schizophrenia.
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GRK2i
0 ImagesCat. No.: HY-P1396CAS No.: 148505-03-7GRK2i 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).
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CCG-273463
0 ImagesCat. No.: HY-150040CAS No.: 2750413-99-9CCG-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.
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C18 LPA
0 ImagesCat. No.: HY-W783254CAS No.: 799279-67-7Synonyms: PA(18:0e/0:0)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.
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Paeoniflorin-6′-O-benzene sulfonate
0 ImagesCat. No.: HY-168971CAS No.: 1390658-79-3Synonyms: CP-25Paeoniflorin-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.
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CCG-224406
0 ImagesCat. No.: HY-123254CAS No.: 1870843-22-3CCG-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.
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GSK466317A
0 ImagesCat. No.: HY-119232CAS No.: 864082-48-4GSK466317A 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.
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Paroxetine-d4 hydrochloride
0 ImagesSynonyms: BRL29060-d4 hydrochloride; BRL29060A-d4Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
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GRL-03022
0 ImagesCat. No.: HY-179707GRL-03022 is a potent, selective and non-covalent G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 of 60 nM. GRL-03022 exhibits >16000-fold selectivity over GRK2 (IC50 > 1000 μM). GRL-03022 can be used for heart failure and cancer research.
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GRK5-IN-3
0 ImagesCat. No.: HY-150021CAS No.: 2410793-22-3GRK5-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.
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FGH31
0 ImagesCat. No.: HY-155099CAS No.: 3033813-47-4FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin.
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CMPD101 hydrochloride
0 ImagesCat. No.: HY-103045ACAS No.: 1941168-71-3CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively).
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GRL-098-22
0 ImagesCat. No.: HY-174256GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC50 values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma.
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Grk2 Rat Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS23286Grk2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Grk2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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GRK6-IN-5
0 ImagesCat. No.: HY-169678CAS No.: 33495-39-5GRK6-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.
