Biological Information
Background Information:
ITK (Interleukin-2-inducible T-cell kinase) is an important member of the Tec family of non-receptor tyrosine kinases that play a central role in signaling through antigen receptors such as the T-cell receptor, B-cell receptor, and Fce.
Family:
Kinase
Sub Family:
TK
Class:
Protein Tyrosine
Protein Name:
ITK
Uniprot Number:
Q08881
Protein Aliases:
Interleukin-2-inducible T-cell kinase|IL-2-inducible T-cell kinase|Kinase EMT|T-cell-specific kinase|Tyrosine-protein kinase Lyk
Gene Name:
ITK
Gene ID:
3702
Gene Aliases:
EMT|PSCTK2|LYK
Accession Number:
NM_005546
Organism:
Human
Construct Details:
352-617 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Itk (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.33 mg/mL myelin basic protein, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.
Substrate:
0.33 mg/mL MBP
Tracer:
33P
ATP Concentration:
[ATP]= 200µM (Km= 264.95µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Staurosporine
Test Sample Requirements:
Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.
Minimum Order Quantity:
2
Turnaround Time
Standard:
6 Business Days
Service Scheduling Note:
Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Pulmonology
Adverse / Beneficial Action:
Inhibition of ITK (EMT, LYK, PSCTK2) may be useful in the treatment of allergic airway inflammation and asthma.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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