Tyk2 JH2 Pseudokinase Domain Assay Service
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Target
Tyk2 JH2 Pseudokinase Domain
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Description
Screening and/or profiling inhibitor compounds against TYK2 JH2 Pseudokinase domain ligand binding in a biochemical assay.
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Synonyms
IMD35 assay, JTK1 assay kit, tyrosine kinase 2 kit, Non-receptor tyrosine-protein kinase biochemical assay kit, JAK family
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
Fluorescence Polarization
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Reference Compounds and IC50
BMS-986165, 0.018 μM
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Assay Principle
The TYK2 JH2 Pseudokinase Domain Inhibitor Screening Assay is designed for screening and profiling small molecules that displace the fluorescently labeled probe (JH2 probe 1) from the JH2 domain of TYK2. The assay is based on the competition of the test compound with the JH2 probe for binding to purified TYK2 JH2. Using this kit, only one simple step on a microplate is required for screening. The JH2 probe 1 is incubated with a sample containing TYK2 JH2 to produce a change in fluorescent polarization.
Target Details
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Protein Family
Kinases
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UniProt
P29597
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Background
Janus kinases (JAKs) are a family of intracellular nonreceptor tyrosine kinases including Jak1, Jak2, Jak3 and TYK2, that has been recognized as an important modulator in inflammatory processes. JAKs contain a catalytically inactive pseudokinase regulatory domain (JH2) as well as an active kinase domain (JH1). Selective inhibition of one specific Jak is a challenging task since the enzymes share high homology in the active site of JH1. Recent reports demonstrate that the pseudokinase domain (JH2) could provide an ideal allosteric site for selective inhibitor development.
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.
