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Pathways Recommended: GPCR/G Protein
Results for "

G protein-coupled receptor kinase

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

2

Peptides

1

Recombinant Proteins

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-W036034A
    GRK-IN-1

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
    GRK-IN-1
  • HY-123520
    GSK299115A

    		G Protein-coupled Receptor Kinase (GRK) PKA Cancer
    GSK299115A is a G Protein-coupled Receptor Kinase (GRK) and PKA inhibitor .
    GSK299115A
  • 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-18990
    GSK180736A
    4 Publications Verification

    		 ROCK Cardiovascular Disease
    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-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-142817
    GRK6-IN-2

    		G Protein-coupled Receptor Kinase (GRK) Cancer
    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-142812
    GRK6-IN-1

    		G Protein-coupled Receptor Kinase (GRK) Cancer
    GRK6-IN-1 (compound 18) 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-1 has the potential for the research of multiple myeloma .
    GRK6-IN-1
  • 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-123538
    GRK2 Inhibitor 1

    		Others Cardiovascular Disease
    GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a GRK2 (β-ARK1) inhibitor .
    GRK2 Inhibitor 1
  • 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-W013411
    (E/Z)-Locostatin

    (E/Z)-UIC-1005

    		 Others Cancer
    (E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. 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 aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
    (E/Z)-Locostatin
  • HY-W013411A
    Locostatin

    UIC-1005

    		 Others Cancer
    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-128311
    GRK6-IN-3

    		G Protein-coupled Receptor Kinase (GRK) Inflammation/Immunology
    GRK6-IN-3 is a G protein coupled receptor 6 kinase (GRK6) inhibitor with an IC50 1.03 μM .
    GRK6-IN-3
  • HY-P1396
    GRK2i

    		G Protein-coupled Receptor Kinase (GRK) Others
    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-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-15589
    GW9508
    4 Publications Verification

    		 Free Fatty Acid Receptor Potassium Channel Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
    GW9508
  • 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-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-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-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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