SRP5034

GRK2, active, GST tagged human

PRECISIO^® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution

• Synonym(e): β-ARK1, ADRBK1, BARK1, FLJ16718
• NACRES: NA.77
• UNSPSC Code: 12352200
• Specific activity: 4.5-6.1 nmol/min·mg
• Assay: ≥70% (SDS-PAGE)
• Recombinant: expressed in baculovirus infected Sf9 cells

Eigenschaften

• recombinant: expressed in baculovirus infected Sf9 cells
• product line: PRECISIO^® Kinase
• assay: ≥70% (SDS-PAGE)
• form: buffered aqueous glycerol solution
• specific activity: 4.5-6.1 nmol/min·mg
• mol wt: ~102 kDa
• NCBI accession no.: NM_001619
• shipped in: dry ice
• storage temp.: −70°C
• Gene Information: human ... ADRBK1(156)

Beschreibung

General description

G-protein-coupled receptor kinase 2 (GRK2), which is officially known as adrenergic, beta, receptor kinase 1 (ADRBK1), gene codes for a 689 amino acid protein, that is of 79.573kDa. This gene has 12 catalytic region subdomains. GRK2 is expressed in the vascular endothelium, arterial smooth muscle, myocardium, kidney and in the renal proximal tubule. It is mapped to human chromosome 11q13.

Biochem/physiol Actions

G-protein-coupled receptor kinase 2 (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. RAF kinase inhibitor protein RKIP is a physiologic inhibitor of GRK2. After stimulation of G protein-coupled receptors, RKIP dissociates from its known target, RAF1 to associate with GRK2 and block its activity. G-protein-coupled receptor kinase 2 (GRK2) controls several intracellular mechanisms. It helps to maintain the structure and activities of the heart. Hence it participates in several cardiovascular diseases. GRK2 also modulates ion and fluid transport and eventually, blood pressure. It increases the synthesis of mitochondrial superoxide and reduces oxygen utilization and ATP synthesis. This protein serves as a major onco-modulator.

Physical form

Supplied in 50mM Tris-HCl, pH 7.5, 150mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25mM DTT, 0.1mM PMSF, 25% glycerol.

Preparation Note

after opening, aliquot into smaller quantities and store at -70 °C. Avoid repeating handling and multiple freeze/thaw cycles

Legal Information

PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklasse: 10 - Combustible liquids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable