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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: MINK1 (misshapen/NIK related kinase 1), also known as MAPK4K6, is a serine/threonine kinase member of the germinal center kinase (GCK) family that are homologous to the Ste20 family and regulate a wide variety of cellular processes, including thymocyte selection and platelet function. It is found at high levels in myeloid and dendritic cells. It plays a role in tumor immunity by acting on the Hippo pathway and by activation of LATS1/2 (large tumor suppressor kinase 1/2). It can regulate planner cell polarity by forming a complex with PRICKLE1 (prickle planar cell polarity protein 1), and Rictor (rapamycin-insensitive companion of mammalian target of rapamycin) that regulates AKT-dependent cell migration. MINK1 is also involved in resistance to 5FU (5-fluorouacil), a chemotherapy medication, in OSCC (oral squamous cell carcinoma), by modulating the levels of p53. The presence of ROS (reactive oxygen species) activates MINK1, which can phosphorylate Ser725 on NLRP3 (NOD-, LRR- and pyrin domain-containing protein 3) and contribute to inflammatory diseases. The use of ROS scavengers can alleviate the activation of the inflammasome via MINK1 activity disruption. MINK1 deficiency plays conflicting roles in the degeneration of joints due to aging or injury. It has also been shown to protect cartilage tissue from degenerating in aging joints via SMAD2 (mothers against decapentaplegic homolog 2) activation in chondrocytes, but in the case of injury it aggravates OA (osteoarthritis). A deeper understanding of the roles played by this protein in different contexts will help us understand how best to modulate its activity to bring health benefits.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ MINK1 Kinase Assay Kit is designed to measure MINK1 (misshapen/NIK-related kinase 1) 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 MINK1 (amino acids 1-320), 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: Q8N4C8
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Hu Y., et al., 2004 J Biol Chem. 279(52):54387-97.
Nicke B., et al., 2005 Mol Cell. 20(5):673-85.
Yu D., et al., 2020 Osteoarthritis Cartilage 28(10:112-121.
Zhu K., et al., 2021 Cell Mol Immunol 18(10):2372-2382.
Mohanty S., et al., 2022 Oncogene 41:4929-4940.
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