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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: MAPKAPK2, or MAP kinase-activated protein kinase 2, is a serine/threonine kinase protein. MAPKAPK2 is phosphorylated by p38 MAP kinase (p38MAPK) and participates in multiple crucial cellular pathways: stress response, cell cycle, cell apoptosis and inflammatory responses. One of its main substrates is HSP27 (heat shoch protein 27), a protein involved in oxidative stress responses, but can also activate and inactivate RNA-binding proteins (RBPs). By acting on RBPs it can regulate the expression of proto-oncogenes, cytokines, chemokines, and pro-inflammatory factors. It has been implicated in colorectal, skin, bladder and prostate cancer, and inflammatory diseases. The use of p38MAPK inhibitors can lead to hepatic and cardiac toxicology and central nervous disorders likely because p38MAPK can interact with more than 60 partners involved in multiple pathways. MAPKAPK2 can be seen as a cell-cycle checkpoint and has become an attractive target for combination-based therapies in cancer. It has also been considered a disease-modifying anti-rheumatic drug (DMARD) ligand, and inhibitors of MAPKAPK2 may prove beneficial for the treatment of inflammatory diseases such as rheumatoid arthritis.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ MAPKAPK2 Kinase Assay Kit is designed to measure MAPKAPK2 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 MAPKAPK2 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: P49137
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Soni S., et al., 2019 Journal of Experimental & Clinical Cancer Research 38: 121.
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