SRP5034
GRK2, active, GST tagged human
PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution
Synonyme(s) :
β-ARK1, ADRBK1, BARK1, FLJ16718
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About This Item
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77
Produit recombinant
expressed in baculovirus infected Sf9 cells
Gamme de produits
PRECISIO® Kinase
Pureté
≥70% (SDS-PAGE)
Forme
buffered aqueous glycerol solution
Activité spécifique
4.5-6.1 nmol/min·mg
Poids mol.
~102 kDa
Numéro d'accès NCBI
Conditions d'expédition
dry ice
Température de stockage
−70°C
Informations sur le gène
human ... ADRBK1(156)
Description générale
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.
Actions biochimiques/physiologiques
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.
Forme physique
Supplied in 50mM Tris-HCl, pH 7.5, 150mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25mM DTT, 0.1mM PMSF, 25% glycerol.
Notes préparatoires
after opening, aliquot into smaller quantities and store at -70 °C. Avoid repeating handling and multiple freeze/thaw cycles
Informations légales
PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
10 - Combustible liquids
Classe de danger pour l'eau (WGK)
WGK 1
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".
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Kristina Lorenz et al.
Nature, 426(6966), 574-579 (2003-12-05)
Feedback inhibition is a fundamental principle in signal transduction allowing rapid adaptation to different stimuli. In mammalian cells, the major feedback inhibitor for G-protein-coupled receptors (GPCR) is G-protein-coupled receptor kinase 2 (GRK-2), which phosphorylates activated receptors, uncouples them from G
H A Rockman et al.
Proceedings of the National Academy of Sciences of the United States of America, 95(12), 7000-7005 (1998-06-17)
Heart failure is accompanied by severely impaired beta-adrenergic receptor (betaAR) function, which includes loss of betaAR density and functional uncoupling of remaining receptors. An important mechanism for the rapid desensitization of betaAR function is agonist-stimulated receptor phosphorylation by the betaAR
G-protein-coupled receptor kinase 2 (GRK2) inhibitors: current trends and future perspectives
Guccione M, et al.
Journal of Medicinal Chemistry, 59(20), 9277-9294 (2016)
G protein-coupled receptor kinases: Crucial regulators of blood pressure
Yang J, et al.
Journal of the American Heart Association, 5(7), e003519-e003519 (2016)
G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a HDAC6-Pin1 axis
Nogues LR, et al.
EBioMedicine, 13, 132-145 (2016)
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