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Applications: Useful for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Background: The pyruvate dehydrogenase (PDH) complex is a mitochondrial complex that converts pyruvate to acetyl-CoA. It is a primary regulator of glucose metabolism by providing the link between glycolysis and the tricarboxylic acid cycle. The enzymatic activity of PDH is regulated by a phosphorylation/dephosphorylation cycle, in which phosphorylation results in inactivation of PDH. PDK3 inhibits the PDH complex by phosphorylation of the E1 alpha subunit.PDK3 participates in the metabolic switch of cancer cells; although its significance in tumor malignancy is unknown. PDK3 has been implicated in drug resistance following the treatment of leukemia or colon cancer.
Description: The PDK3 Kinase Assay Kit is designed to measure PDK3 activity for screening and profiling applications using ADP-Glo® as a detection reagent. The signal is measured using a luminometer or a microplate reader capable of reading chemiluminescence.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Supplied As: The PDK3 Kinase Assay Kit comes in a convenient 96-well format, with enough purified PDK3, Casein, ATP, and kinase assay buffer for 96 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Feng, Lan, et al. "miR-497-5p inhibits gastric cancer cell proliferation and growth through targeting PDK3." Bioscience Reports9 (2019): BSR20190654.
2. Lu, Chun-Wun, et al. "Overexpression of pyruvate dehydrogenase kinase 3 increases drug resistance and early recurrence in colon cancer." J. Pathol. 179.3 (2011): 1405-1414.
3. Mohammad, Taj, et al. "Identification of high-affinity inhibitors of pyruvate dehydrogenase kinase-3: Towards therapeutic management of cancer." Biomolec. Struct. Dynam. 39.2 (2021): 586-594.
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