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

PubChem ID

122130844

Name

Staurosporine

Measurement

37.67nM - IC50

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

RELATED SOLUTIONS

Item: 14-660KP10