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Application: 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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