OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
BTK (Bruton’s Tyrosine Kinase) is a member of the Tec family kinases which are important components of both antigen receptor signaling and other cell surface receptors, resulting in regulation of the actin cytoskeleton, adhesion, migration, and transcriptional activation. BTK is found in all cells of the hematopoietic lineage except plasma and T cells, and is required for normal B cell development and signal transduction through cell surface molecules. Mutations in the btk gene result in aberrant B cell development, leading to the X-linked agammaglobulinemia phenotype in humans and to the less severe X-linked immunodeficiency in mice. BTK inhibitors may be of benefit in the treatment of leukemias and lymphomas.
Family:
Kinase
Sub Family:
TK
Class:
Protein Tyrosine
Protein Name:
BTK
Uniprot Number:
Q06187
Protein Aliases:
Bruton's tyrosine kinase
Gene Name:
BTK
Gene ID:
695
Gene Aliases:
ATK|XLA|PSCTK1
Accession Number:
NM_000061
Organism:
Human
Construct Details:
Full length; R28H recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
BTK (R28H) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 1% Triton X-100, 300 µM LSNLYHQGKFLQTFCGSPLYRRR, 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:
300 µM LSNLYHQGKFLQTFCGSPLYRRR
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 292µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
Acid Blank
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
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
BTK Human TK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-552KP
BTK Human TK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-552KP10
BTK (R28H) Human TK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-765KP
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