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Application: Study enzyme kinetics and screen small molecular inhibitors for drug discovery and high throughput (HTS) applications.
Background: FAK (focal adhesion kinase) is a non-receptor tyrosine kinase present in the cytoplasm and involved in crucial cellular functions, such as adhesion, proliferation and survival. It works as a mediator of signals between the ECM (extracellular matrix) and the cytoplasm, and when activated can have kinase-dependent and kinase-independent activity. It is found at high levels in many cancer types, including breast and ovarian cancer. For instance, in breast cancer cells, it was found that disruption of the FAK-mediated signaling pathways can result in increased FADD (Fas-associated death domain) and caspase-8 activity and apoptosis. In addition to its role in apoptosis, it is also involved in EMT (epithelial-mesenchymal transition), cell migration, and regulation of the TME (tumor microenvironment). Its importance in cancer development makes it an attractive target in cancer therapy, with multiple inhibitors undergoing clinical and pre-clinical studies. The use of combination therapy of inhibitors for FAK with immune checkpoint inhibitors like PD-L1, chemotherapy, and radiotherapy, may lead to better outcomes than individual approaches and may open new therapeutic avenues in cancer.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ FAK Kinase is designed to measure FAK (focal adhesion kinase) 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 recombinant FAK kinase (amino acids 411-686), kinase substrate, ATP and kinase assay buffer for 100 enzyme reactions.
Genbank: L13616
Storage Stability: Store at -80°C. This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: Q05397
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Tan X., et al., 2023 Experimental Hematology & Oncology 12:83.
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