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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: TTBK1, also known as tau tubulin kinase 1, is a member of the serine/threonine kinase family and belongs to the CK-1 (casein kinase 1) super-family. TTBK1, contrary to the isoform TTKB2, has a restricted pattern of expression and is involved in the phosphorylation of tau, tubulin and TPD-43. TTBK1 phosphorylates tau in cortical neurons, on the epitopes that are found enriched in tauopathies, such as Alzheimer's disease (AD) and amyotrophic lateral sclerosis. Despite its close similarity to TTBK2, each protein phosphorylates specific partners and is involved in specific pathways. The TTBK1 inhibitor, named 31, was able to reach the CNS (central nervous system) and inhibit tau phosphorylation on the Ser 422 epitope in mouse and rat animal models, making it an interesting inhibitor for the treatment of AD. The development of inhibitors specific for TTBK1 is challenging, but the treatment of neurodegenerative diseases linked to aging is crucial as human life expectancy increases.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ TTBK1 Kinase Assay Kit is designed to measure TTBK1 (tau-tubulin kinase 1) 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 TTBK1 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: Q5TCY1
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Nozal V. and Martinez A., 2019 Eur J Med Chem 161:39-47.
Bao C., et al., 2021 Cell Mol Neurobiol 41(4): 669-685.
Halkina T., et al., 2021 J Med Chem 64 (9): 6358-6380.
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