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GRK

G protein-coupled receptor kinases (GRKs, GPCRKs) are a family of protein kinases within the AGC (protein kinase A, protein kinase G, protein kinase C) group of kinases. Like all AGC kinases, GRKs use ATP to add phosphate to Serine and Threonine residues in specific locations of target proteins. In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways.

  • GSK299115A
    T27471864082-35-9In house
    GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.
    • $336
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  • GSK270822A
    T27467864082-23-5In house
    GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.
    • $238
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  • 1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID
    T8913260555-42-8
    1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.
    • $50
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  • Paroxetine hydrochloride
    T163678246-49-8
    Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.
    • $45
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    TargetMol | Citations Cited
  • GRK6-IN-1
    T625182677786-61-5
    GRK6-IN-1 is a selective and potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) (IC50: 120 nM).GRK6-IN-1 is useful for the study of multiple myeloma and triple-negative breast cancer.
    • $52
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    TargetMol | Inhibitor Sale
  • GRK5-IN-2
    T96091642839-27-7
    GRK5-IN-2, a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. It regulates the expression and/or release of insulin and is useful for the metabolic disease research.
    • $33
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    TargetMol | Inhibitor Sale
  • GRK2-IN-1 hydrochloride (2055990-90-2 free base)
    T13714L
    GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
    • $108
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    TargetMol | Inhibitor Sale
  • CMPD101
    T14989865608-11-3
    CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2 3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. 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.
    • $60
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  • CCG258208
    T137142055990-90-2
    GRKs-IN-1 has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).
    • $2,420
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  • Takeda103A
    T24850865609-72-9
    Takeda103A (CMPD103A) is the GRK2-dependent bovine tubulin oxidation effective inhibitor.
    • $129
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  • CCG215022
    T34981813527-81-9
    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, 5 and 1, respectively.
    • $97
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    TargetMol | Inhibitor Sale
  • GSK180736A
    T3513817194-38-0
    GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
    • $35
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  • GRK6-IN-2
    T615562677786-27-3
    GRK6-IN-2 is a potent G protein-coupled receptor kinase 6 (GRK6) inhibitor with potential antitumor activity.GRK6-IN-2 has been studied in multiple myeloma.
    • $56
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