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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: In mammals, there are four JAK tyrosine kinases: JAK1, JAK2, JAK3 and TYK2. They are found in the cytosol. JAK3 is involved in signaling in response to cytokine activation of type I receptors that have γc chains (such as IL-2R, IL-21R and IL-15R). JAK3 plays roles in cell growth, survival, differentiation and EMT (epithelial to mesenchymal transition), and can be found in T cells, NK cells and intestinal epithelial cells. Inactive JAK3 results in SCID (severe combined immunodeficiency disease), while hyperactivation can lead to cancer and autoimmune disorders. Activated JAK phosphorylates tyrosine residues in the receptor, allowing the binding of STAT (signal transduction and activators of transcription) and their phosphorylation. Phosphorylated STAT factors dimerize and move to the nucleus where they regulate specific gene expression. The JAK3 inhibitor tofacitinib is in clinical trial for the treatment of psoriasis and organ rejection after transplant, and it is commercially available for rheumatoid arthritis. The development of new JAK3-related therapies will open new therapeutic avenues in cancer and autoimmune disorders.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ JAK3 Kinase Assay Kit is designed to measure JAK3 (Janus Kinase 3) 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 JAK3 (amino acids 811-1124), 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: P52333
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Shawky A., et al., 2022 Pharmaceutics 14(5):1001.
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