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 (64)
Related Products (64)
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Antibodies (2)
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KR-39038
0 ImagesKR-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.
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GRL018-21
0 ImagesCat. No.: HY-149720CAS No.: 3061801-07-5GRL018-21 is a potent and highly selective G protein-coupled receptor kinase 5 (GRK5) inhibitor with an IC50 value of 10 nM.
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Anti-GPR20 Antibody
0 ImagesCat. No.: HY-P990578Purity: 99.78%Synonyms: DS-6157 antibodyAnti-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).
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GRK2 degrader-1
0 ImagesGRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research.
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IS20
0 ImagesIS20 is a Prokineticin receptor 1 (PKR1) agonist. IS20 diminishes Doxorubicin (HY-15142A) mediated apoptosis and ROS production by activating Akt or MAPK pathways. IS20 protects the heart against Doxorubicin-induced cardiovascular toxicity and improves the survival rate and cardiac function in mouse models. IS20 does not alter the cytotoxicity and antitumor activity of acute DOX treatment in breast cancer cells and MDA-MB-231 xenograft mouse models. IS20 can be used for cancers research.
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GRL093-22
0 ImagesGRL093-22 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.
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GRK-IN-1
0 ImagesCat. No.: HY-W036034ACAS No.: 5423-98-3GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
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Takeda103A
0 ImagesTakeda103A 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.
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GRK2 Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS05813GRK2 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.
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CCG258208
0 ImagesCat. No.: HY-109562CAS No.: 2055990-90-2Synonyms: GRKs-IN-1CCG258208 (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.
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GRK6-IN-3
0 ImagesCat. No.: HY-128311CAS No.: 499231-87-7GRK6-IN-3 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 1.03 μM.
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Paroxetine hydrochloride hemihydrate (Standard)
0 ImagesSynonyms: BRL29060 hydrochloride hemihydrate (Standard); BRL29060A hemihydrate (Standard)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.
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Corazonin
0 ImagesCat. No.: HY-P3035CAS No.: 122929-08-2Corazonin 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.
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CCG 224061
0 ImagesCat. No.: HY-120718CAS No.: 2055990-82-2CCG 224061 is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with a IC50 of 0.066 μM. CCG 224061 inhibits GRK activity in cardiomyocytes. CCG 224061 is applicable to research related to heart disease, heart failure, myocardial hypertrophy and hypertension.
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GSK317354A
0 ImagesCat. No.: HY-111239CAS No.: 874119-13-8GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.
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Gαi2-IN-1
0 ImagesCat. No.: HY-176780CAS No.: 2794979-74-9Gαi2-IN-1 is a Gαi2 inhibitor. Gαi2-IN-1 attenuates migration of prostate cancer cells. Gαi2-IN-1 can be used for the research of prostate cancer .
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LAS195319
0 ImagesCat. No.: HY-123862CAS No.: 1605328-04-8LAS195319 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).
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CCG-271423
0 ImagesCat. No.: HY-150039CAS No.: 2750413-88-6CCG-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.
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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).
