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Description
for screening/characterizing/studying potential inhibitors of Human PEPCK1
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Summary
Phosphoenolpyruvate Carboxykinase (PEPCK, EC 4.1.1.32) is an enzyme, which belongs to the lyase family. In the presence of GTP, it catalyzes the reversible conversion of oxaloacetate (OAA) into phosphoenolpyruvate (PEP), GDP and CO2. In humans, two isoforms of PEPCK are found: cytosolic form (PEPCK-C, PEPCK1 or PCK1) and mitochondrial form (PEPCK-M). PEPCK1 is a rate-controlling step in gluconeogenesis and a key gluconeogenic enzyme in liver and kidney. Recent studies have shown that overexpressing of PEPCK1 in liver leads to excessive glucose production and type II diabetic phenotype in mice. Therefore, identifying and screening PEPCK1 inhibitors is a useful strategy for the treatment of type II diabetes and obesity. In BioVision’s Human Phosphoenolpyruvate Carboxykinase 1 Inhibitor Screening Kit, PEPCK1 is coupled with a set of enzymes that covert PEP and carbonate into a series of intermediates and hydrogen peroxide, which in turn reacts with a probe thereby generating a colorimetric signal (OD 570 nm). In the presence of PEPCK1 Inhibitor, the reaction is impeded. A PEPCK1 Inhibitor Control is included to compare the efficacy of the sample inhibitors. The assay is high-throughput adaptable and can be completed in less than 1 hr.
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Detection Method
Absorbance, OD 570 nm
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Species Reactivity
Mammalian
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Applications
Screening/characterizing/studying potential inhibitors of Human PEPCK1
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Sample Type
Test compounds
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Features Benefits
High-throughput adaptable, Simple, Quick
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Storage Conditions
-20°C
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Shipping Conditions
Gel Pack
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Shelf life
12 months
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Background
Phosphoenolpyruvate Carboxykinase (PEPCK, EC 4.1.1.32) is an enzyme, which belongs to the lyase family. In the presence of GTP, it catalyzes the reversible conversion of oxaloacetate (OAA) into phosphoenolpyruvate (PEP), GDP and CO2. In humans, two isoforms of PEPCK are found: cytosolic form (PEPCK-C, PEPCK1 or PCK1) and mitochondrial form (PEPCK-M). PEPCK1 is a rate-controlling step in gluconeogenesis and a key gluconeogenic enzyme in liver and kidney. Recent studies have shown that overexpressing of PEPCK1 in liver leads to excessive glucose production and type II diabetic phenotype in mice. Therefore, identifying and screening PEPCK1 inhibitors is a useful strategy for the treatment of type II diabetes and obesity. In BioVision’s Human Phosphoenolpyruvate Carboxykinase 1 Inhibitor Screening Kit, PEPCK1 is coupled with a set of enzymes that covert PEP and carbonate into a series of intermediates and hydrogen peroxide, which in turn reacts with a probe thereby generating a colorimetric signal (OD 570 nm). In the presence of PEPCK1 Inhibitor, the reaction is impeded. A PEPCK1 Inhibitor Control is included to compare the efficacy of the sample inhibitors. The assay is high-throughput adaptable and can be completed in less than 1 hr.
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
