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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 processes. JAKs contain a catalytically inactive pseudokinase regulatory domain (JH2), that acts as a negative regulator, as well as an active kinase domain (JH1). Most of the mutations in JAK proteins that link to hematological and immune-related diseases occur in the JH2 domain, resulting in increased JAK2 activity or decreased cytokine-induced signaling. In 2005 the JAK2 V617F mutation was identified in myeloproliferative neoplasm (MNPs), and nearly all patients with polycythemia vera have mutations in JAK2. 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™ JAK2 Kinase Assay Kit is designed to measure JAK2 (Janus Kinase 2) 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 JAK2 (JH1 domain) (amino acids 808-1132), 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: O60674
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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