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Encompassing Amino Acids: full length
Applications: Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.
Background: GRK2 or ADRBK1 is a ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G protein-coupled receptors. GRK2 phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart (1). RAF kinase inhibitor protein RKIP is a physiologic inhibitor of GRK2 (2). After stimulation of G protein-coupled receptors, RKIP dissociates from its known target, RAF1 to associate with GRK2 and block its activity.
Description: Recombinant human GRK2, full length, with N-terminal GST-tag, expressed in Sf9 insect cells via a baculovirus expression system.
Format: Aqueous buffer solution
Formulation: 50 mM Tris-HCl, pH 7.5, 150 mM NaCl, 10 mM glutathione, 0.1 mM EDTA, 0.25 mM DTT, 0.1 mM PMSF, 25% glycerol
Genbank: NM_001619
Host Cell Line: Sf9 cells
Purity: ≥90%
Storage Stability: At least 6 months at -80°C.
Tags: N-terminal GST-tag
Uniprot: P25098
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Rockman, H. A. et al: Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice. Proc. Nat. Acad. Sci. 95: 7000-7005, 1998.
2. Lorenz, K. et al: Protein kinase C switches the Raf kinase inhibitor from Raf-1 to GRK-2. Nature 426: 574-579, 2003.
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