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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: TNIK (TRAF2 and NCK interacting kinase) is a serine-threonine kinase of the GCK (germinal center kinase) family of proteins. It is characterized by an N-terminal kinase domain and a C-terminal GCK domain that serves a regulatory function. It is a specific effector of RAP2 (RAP2A, member of RAS oncogene family), which regulates the actin cytoskeleton, and can activate the JNK (c-Jun N-terminal kinase) pathways. It can also interact with TCF4 and β-catenin and activate Wnt signaling. It has been linked to cancer, and it is known that colorectal cancer is highly dependent on this protein. The development of inhibitors targeting TNIK has been ongoing for more than 10 years, focusing on the ATP-binding site. NCB-0846 has anti-Wnt signaling and anti-tumorigenesis activities and is a promising colorectal therapeutic. Recently, generative AI identified TNIK as a target for anti-fibrotic drug development, with the inhibitor INS018_55 showing selective and anti-fibrotic activity in animal models. This finding opens the possibility of using TNIK inhibitors for IPF (idiopathic pulmonary fibrosis) and CKD (chronic kidney disease).
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ TNIK Kinase Assay Kit is designed to measure TNIK (TRAF2 and NCK interacting kinase) 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 TNIK, 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: Q9UKE5
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Kukimoto-Niino M., et al., 2022 Int J Mol Sci 23(21):13010.
Ren F., et al., 2024 Nat Biotechnol: doi.org/10.1038/s41587-024-02143-0.
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