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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: c-Met (mesenchymal-epithelial transition), also known as HGFR (hepatocyte growth factor receptor), is a receptor tyrosine kinase (RTK) encoded by the gene MET. It is formed as a single chain precursor that undergoes proteolytic cleavage to form a glycosylated heterodimer. Upon binding the ligand HGF (hepatocyte growth factor), c-Met forms a dimer that can undergo autophosphorylation and activates the MAPK (mitogen-activated protein kinase) signaling pathway, and thus multiple cellular processes including proliferation, adhesion, angiogenesis and EMT (epithelial-mesenchymal transition). Importantly, c-Met is overexpressed in various carcinomas, suggesting that the HGF/c-Met signaling pathway could be a promising target for cancer treatment. A splice mutation that results in skipping exon 14 has been identified in the tumor tissue of approximately 4% of patients with lung cancer, particularly those with non-small cell lung cancer (NSCLC). This mutation causes over-expression of MET protein and increased MET activation, leading to oncogenesis. Interestingly, it also seems to be required for neutrophil cytotoxicity, and so its inhibition also impacts the role of neutrophils in cancer treatment. Further studies into the role of this protein and strategies to target it will open new therapeutic avenues in oncology.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ c-MET Kinase Assay Kit is designed to measure c-MET (mesenchymal-epithelial transition) tyrosine 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 c-MET (amino acids 956-1390), 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: P08581
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Recondo G., et al., 2020 Cancer Discov. 10(7): 922-934.
Awad M.M., et al., 2016 J. Clin. Oncology 34: 721-30.
Faiella A., et al., 2022 J Oncol: 5179182.
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