OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Myotonic dystrophy (DM1) is the most common form of muscular dystrophy in adults, caused by amplification of an unstable (CTG)n repeat in the 3' untranslated region (3'-UTR) of the DM1 protein kinase (DMPK) gene. Myotonic dystrophy protein kinase (DMPK) is a serine threonine kinase encoded by the DM-1 locus.
Family:
Kinase
Sub Family:
AGC
Class:
Protein Ser/Thr
Protein Name:
DMPK
Uniprot Number:
Q09013
Protein Aliases:
dystrophia myotonica 1|DM protein kinase|myotonin protein kinase A|myotonic dystrophy associated protein kinase|thymopoietin homolog
Gene Name:
DMPK
Gene ID:
1760
Gene Aliases:
DMK|DM1PK|MDPK|MT-PK
Accession Number:
NM_004409
Organism:
Human
Construct Details:
1-549 recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
DMPK (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100, 250 µM KKSRGDYMTMQIG, 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:
250 uM KKSRGDYMTMQIG
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 9.21µM )
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:
Permanent overexpression of DMPK may cause myotonic myopathy, hypertrophic cardiomyopathy with dysrhythmia and hypotension. DMPK inhibition, however, may cause typical myotonic dystrophy symptoms and heart conduction defects.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
DMPK Human AGC Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-649KP10
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