DMPK Human AGC Kinase Enzymatic Radiometric LeadHunter Assay [10 μM ATP] - TW

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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:

Fragment (1-549), Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant protein kinase DMPK expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 37 mU/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 25 µM Axl-tide, 10 µM ATP and 0.25 µCi [γ32P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Axl-tide formed. Compounds are screened at 10 µM.

Substrate:

25 µM Axltide

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

Staurosporine

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

0.0057μM - IC50

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:

Taiwan - Taipei