OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
BRK (breast tumor kinase, PTK6) is a nonreceptor tyrosine kinase containing SH3, SH2, and tyrosine kinase catalytic domains. BRK overexpression is frequently observed in breast cancer and several other cancer types. Studies reveal BRK translocates to membrane ruffles, where it colocalizes with paxillin during cell migration. Inhibition of BRK may be useful for the treatment of breast and other cancers.
Family:
Kinase
Sub Family:
TK
Class:
Protein Tyrosine
Protein Name:
Brk (PTK6)
Uniprot Number:
Q13882
Protein Aliases:
Breast tumor kinase|Tyrosine-protein kinase BRK
Gene Name:
PTK6
Gene ID:
5753
Gene Aliases:
BRK
Accession Number:
NM_005975
Organism:
Human
Construct Details:
Full length recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
BRK (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2, 0.1 mg/mL poly (Glu,Tyr) 4:1, 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 ethanol prior to drying and scintillation counting.
Substrate:
0.1 mg/mL poly (Glu,Tyr)
Tracer:
33P
ATP Concentration:
[ATP]= 15µM (Km= 28µM )
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:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibition of BRKmay be useful for thetreatment of breast and other cancers.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
Brk (PTK6) Human TK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-613KP10
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