JAK1 Assay Service
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Target
JAK1
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Description
Screening and/or profiling inhibitor compounds against JAK1 kinase activity in a biochemical assay.
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Synonyms
Tyrosine-protein kinase JAK1, JAK-1, JAK1A, JAK1B
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
Luminescent
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Reference Compounds and IC50
Staurosporine, 3 nM
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Assay Principle
The JAK1 (Janus Kinase 1) Assay is designed to measure JAK1 activity for screening and profiling applications using Kinase-Glo® MAX as a detection reagent.
Target Details
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Protein Family
Kinases
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UniProt
P23458
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Background
Janus kinases (JAKs) are a family of intracellular non-receptor 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. 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), while generating minimal side effects. The development of such inhibitors will open new avenues in cancer therapy.
Delivery
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Estimated Turnaround
Two to three weeks following delivery of compounds
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Results
Extensive report with raw and analyzed data, graphs, and detailed protocols. Includes positive control for inhibition.
