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GRK5 inhibitor

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17

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149720
    GRL018-21

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-136561
    GRK5-IN-2

    		G Protein-coupled Receptor Kinase (GRK) Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research .
    GRK5-IN-2
  • HY-47573
    CCG273441

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease Cancer
    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-18991
    CCG215022
    3 Publications Verification

    		 PKA Cancer
    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-139690
    CCG258747

    		Opioid Receptor Cardiovascular Disease
    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-150021
    GRK5-IN-3

    		G Protein-coupled Receptor Kinase (GRK) Others
    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-150022
    GRK5-IN-4

    CCG-265328

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-150039
    CCG-271423

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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 Ca 2+ 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-150040
    CCG-273463

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease Cancer
    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-119232
    GSK466317A

    		PKA G Protein-coupled Receptor Kinase (GRK) Neurological Disease Cancer
    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-143248
    KR-39038

    		G Protein-coupled Receptor Kinase (GRK) HDAC Cardiovascular Disease
    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-103045
    CMPD101
    3 Publications Verification

    		 PKC ROCK Cardiovascular Disease
    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-109562
    CCG258208

    GRKs-IN-1

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-109562A
    CCG258208 hydrochloride

    GRK2-IN-1 hydrochloride

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-118046
    GSK2163632A

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that may serve as a probe for studying heart failure and Parkinson's disease. Screening of known protein kinase inhibitors by differential scanning fluorescence method revealed that the melting points of GRK2 and GRK5 increased. Enzymatic assays of the 14 most stable hits revealed that three exhibited nanomolar inhibitory potency against a single GRK, with some showing significant selectivity. Most of the identified compounds can be divided into two categories: indazole/dihydropyrimidine compounds selectively inhibit GRK2, and pyrrolopyrimidine compounds effectively inhibit GRK1 and GRK5 but with modest selectivity. The two most inhibitory representative compounds, GSK180736A and GSK2163632A, are co-crystals with GRK2 and GRK1, respectively, and their atomic structures were determined to 2.6 and 1.85 ? distances, respectively. GSK180736A, as an inhibitor of Rho-related coiled-coil protein kinase, binds to GRK2 in a manner similar to paroxetine, while GSK2163632A, as an inhibitor of insulin-like growth factor 1 receptor, occupies a novel region of the GRK active site cleft and may be used to achieve more Selectivity. However, both compounds inhibited GRK no more potently than their original targets. These data provide a basis for the rational design of more effective and selective GRK inhibitors in the future .
    GSK2163632A
  • HY-108601A
    (S)-Ro 32-0432

    		PKC Neurological Disease Inflammation/Immunology
    (S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
    (S)-Ro 32-0432
  • HY-108601
    (S)-Ro 32-0432 free base

    		PKC Inflammation/Immunology
    (S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .
    (S)-Ro 32-0432 free base

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