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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: MAPKAPK5 (MAP kinase-activated protein kinase 5), also known as MK5 or PRAK (p-38 regulated/activated kinase), is a member of the serine/threonine kinase family involved in cell motility, growth and survival. In response to activation by MAP (mitogen activated protein) kinases, such as MAPK1, ERK3/4 (extracellular signal-regulated kinase 3,4) and p38, MAPKAPK5 is phosphorylated and translocates from the nucleus to the cytoplasm. MAPKAPK5 mutations can result in neurocardiofaciodigital syndrome, a severe developmental disease. A link between low levels of MAPKAPK5 and Alzheimer's disease (AD) has also been proposed. Additionally, it is linked to cancer. It has recently been identified that a TLK1 (tousled-like kinase 1)-MAPKAPK5 signaling axis exists and can be targeted in prostate cancer. Inhibition of TLK1 and/or MAPKAPK5 was able to reduce metastasis in a xenograft mouse model. These findings emphasize the role of MAPKAPK5 in cancer and open the door to new single or combinatory therapies.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ MAPKAPK5 Kinase Assay Kit is designed to measure MAPKAPK5 (MAP kinase activated protein kinase 5) serine/threonine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified recombinant MAPKAPK5 kinase, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: O54992
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Horn D., et al., 2021 Genetics in Medicine 23:679-688.
Maroofian R., et al., 2023 J Med Genet 60(8): 791-796.
Khalil Md, et al., 2022 Mol Oncol 16(13):2537-2557.
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