SRP5034
GRK2, active, GST tagged human
PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution
Sinônimo(s):
β-ARK1, ADRBK1, BARK1, FLJ16718
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About This Item
Código UNSPSC:
12352200
NACRES:
NA.77
Preço e disponibilidade não estão disponíveis no momento.
recombinante
expressed in baculovirus infected Sf9 cells
linha de produto
PRECISIO® Kinase
Ensaio
≥70% (SDS-PAGE)
Formulário
buffered aqueous glycerol solution
atividade específica
4.5-6.1 nmol/min·mg
peso molecular
~102 kDa
nº de adesão NCBI
Condições de expedição
dry ice
temperatura de armazenamento
−70°C
Informações sobre genes
human ... ADRBK1(156)
Descrição geral
G-protein-coupled receptor kinase 2 (GRK2),[1] which is officially known as adrenergic, beta, receptor kinase 1 (ADRBK1),[2] 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.[2]
Ações bioquímicas/fisiológicas
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.[1] 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.[2] This protein serves as a major onco-modulator.[3]
forma física
Supplied in 50mM Tris-HCl, pH 7.5, 150mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25mM DTT, 0.1mM PMSF, 25% glycerol.
Nota de preparo
after opening, aliquot into smaller quantities and store at -70 °C. Avoid repeating handling and multiple freeze/thaw cycles
Informações legais
PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
10 - Combustible liquids
Classe de risco de água (WGK)
WGK 1
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
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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)
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
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