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GRK

GRK inhibitors act on G protein-coupled receptor kinases (GRKs), which phosphorylate activated receptors. The first member, β-adrenergic receptor kinase, was identified in 1986 because it phosphorylates only the agonist-occupied receptor. In 1990 β-arrestin was described as the protein that then binds the receptor and reduces its function. This sequence underlies receptor desensitization and internalization, and it also starts arrestin-dependent signaling. Mammals have seven GRKs, and GRK2 and GRK5 have been studied most closely in heart and metabolic models. CMPD101 inhibits GRK2 and GRK3, while CCG215022 blocks GRK2 and GRK5. GRK5-IN-2 and GRK6-IN-1 are aimed at single family members, and GSK180736A also inhibits Rho-associated protein kinase 1 (ROCK1).

1 Item

  • GRK2i
    Cat. No.
    A60437
    CAS No.
    148505-03-7

    GRK2i

    GRK2i is a selective Gβγ antagonist that inhibits Gβγ-mediated signaling pathways. This peptide corresponds to the Gβγ-binding domain of G-protein-coupled receptor kinase 2 (GRK2), making it a valuable tool for studying G-protein signaling mechanisms. Its application includes investigating the role of Gβγ subunits in various cellular processes and identifying potential therapeutic targets related to G-protein-coupled receptor signaling.

    In stock View Details
    1 mg
    $945.00
    All 1 sizes

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