OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
MARK, MAP/microtubule affinity-regulating kinase, is a family of serine-threonine kinases that phosphorylates the microtubule-associated proteins. There are 4 members in the family, MARK-1 to 4 which phosphorylate Tau and MAP2/4 in the KXGS motif which is included in the microtubule binding domain and reduce their affinity for microtubules which then become more instable.
Family:
Kinase
Sub Family:
CAMK
Class:
Protein Ser/Thr
Protein Name:
MARK3
Uniprot Number:
P27448
Protein Aliases:
C-TAK1|cTAK1|Cdc25C-associated protein kinase 1|ELKL motif kinase 2|EMK-2|Protein kinase STK10|Ser/Thr protein kinase PAR-1|Par-1a|Serine/threonine-protein kinase p78
Gene Name:
MARK3
Gene ID:
4140
Gene Aliases:
CTAK1|KP78|PAR-1A
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:
MARK3(h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 µM KKKVSRSGLYRSPSMPENLNRPR, 10 mM Magnesium acetate 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:
100 µM KKKVSRSGLYRSPSMPENLNRPR
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 5µM )
Incubation:
40 min at Room temperature
Control Inhibitor:
PKR Inhibitor
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:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Ectopic expression of MARKs in CHO cells leads to destabilisation of the microtubule cytoskeleton. The potentialimportance of these kinases is further highlighted since in brain of Alzheimer patients Tau is hyperphosphorylated on KXGS motif, detaches from microtubules and forms Pair Helical Filaments (PHF) that are abnormal aggregates.The inhibitors of MARK will have potential therapeutic utility in Alzheimer diseasese
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
MARK3 Human CAMK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 15-032KP10
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