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Applications: Screening & profiling of small molecules able to displace the JH2 probe 1 from the ATP binding site of JAK1 (JH2 Pseudokinase Domain).
Background: Janus kinases (JAKs) are a family of intracellular non-receptor tyrosine kinases, including JAK1, JAK2, JAK3 and TYK2, 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. Most inhibitors developed so far target the JH1 domain and seem unable to fully treat the disease, while generating significant side effects by suppressing normal cytokine signaling. Recent reports demonstrate that the pseudokinase domain of JH2 could provide an ideal site for selective inhibitor development and support the treatment of diseases like myeloproliferative neoplasms (MNPs), with minimal side effects.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The JAK1 (JH2 Pseudokinase Domain) Inhibitor Screening Assay Kit is a fluorescence polarization-based assay designed for screening and profiling small molecules that displace the fluorescently labeled probe (JH2 probe 1) from the JH2 pseudokinase domain of JAK1. This kit comes in a convenient 384-well format, with enough recombinant human JAK1 (JH2 Pseudokinase Domain), buffer, and fluorescently labeled JH2 probe 1 for 384 reactions.This assay requires a fluorescent microplate reader capable of measuring fluorescence polarization (FP) to read the FP signal. For more information on the principles of FP, visit bpsbioscience.com/pub/media/ebook_pdf/f/p/fp_assays.pdf.The assay is based on the competition between the test compound and the JH2 probe for the purified JAK1 (JH2 Pseudokinase Domain). JH2 probe 1 is incubated with JAK1 (JH2 Pseudokinase Domain) in the presence or absence of inhibitor. When the JH2 probe 1 is bound to the JH2 pseudokinase domain it has high FP due to its restricted movement. A competitive inhibitor prevents the probe from binding to the JH2 pseudokinase domain, therefore most of the probe is in free form and has low FP. Compared to a control without inhibitor, FP decreases proportionally to the inhibitor concentration.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
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