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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: TBK1 (TANK-binding kinase 1) is serine/threonine kinase involved in cell proliferation, apoptosis, autophagy and immune responses. It is a non-canonical IKK (nuclear factor-κB kinase) kinase, that requires autophosphorylation to become active. It can be activated in response to pathogens, inflammatory cytokines and small GTPases such as KRAS (Kirsten rat sarcoma). This protein participates in several pathways by interacting with different adaptor proteins, which determine TBK1 localization, access to substrates, and function. For example, binding to TANK (TRAF family member associated NF-κB activator) determines a perinuclear localization, while binding to AZI2 (5-azacytidine-induced protein 2) moves the protein to the cytosol. In the context of innate immunity, TBK1 mediates IRF3/7 (interferon regulatory factor 3) activation and NF-κB signaling, resulting in cytokine production. TBK1 activity dysfunction can result in autoimmune disorders (like rheumatoid arthritis), neurodegenerative disorders (amyotropic lateral sclerosis) and cancer. The use of inhibitors for TBK1 has been studied as a therapeutic approach for inflammatory disorders and cancer, with momelotinib being tested in clinical trials. Another inhibitor, amlexanox, is being tested in the context of type II diabetes, MASH and obesity.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ TBK1 Kinase Assay Kit is designed to measure TBK1 (TANK-binding 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 recombinant purified TBK1 (amino acids 2-279), 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: Q9UHD2
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Runde A., et al., 2022 J Exp Clin Cancer Res 41(10):135.
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