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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: Janus kinases (JAKs) are a family of intracellular tyrosine kinases, including JAK1, JAK2, JAK3 and TYK2 (tyrosine kinase 2), important in the modulation of inflammatory responses. JAKs contain a catalytically inactive pseudokinase regulatory domain (JH2), that acts as a negative regulator, as well as an active kinase domain (JH1). JAK1 is involved in dermatitis, allergic rhinitis, asthma and IBD (inflammatory bowel disease). Mutations in JAK can result in lymphoma and leukemia. JAK inhibitors can be classified into reversible or irreversible. Reversible inhibitors may be ATP-competitive or allosteric inhibitors. The development of such inhibitors will open new avenues in cancer or autoimmune disease therapy. Ruxolitinib, a JAK inhibitor, has been approved in 2011 for the treatment of myelofibrosis, and later in 2014 for polycythemia vera. More recently, it has been FDA approved for the treatment of acute and chronic GvHD (graft-versus-host disease). However, this compound can also target other kinases, such as CHK2 (checkpoint kinase 2). The development of highly specific inhibitors will benefit patients suffering from auto-immune disorders and cancer.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ JAK1 Kinase Assay Kit is designed to measure JAK1 (Janus kinase 1) 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 JAK1 (amino acids 866-1154), 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: P23458
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Newton A. S., et al., 2017 ACS Med Chem Lett 8 (6): 614-617.
Wrobleski S. T., et al., 2019 J Med Chem 62 (20): 8973-8995.
Shawky A., et al., 2022 Pharmaceutics 14(5):1001.
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