OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
MARK (MAP/microtubule affinity-regulating kinase) phosphorylates the microtubule-associated proteins tau, MAP2, and MAP4 on their microtubule-binding domain, causing their dissociation from microtubules and increased microtubule dynamics. Overexpression of MARK1 or MARK2 in cells leads to hyperphosphorylation of MAPs and to disruption of the microtubule array, resulting in morphological changes and cell death.
Family:
Kinase
Sub Family:
CAMK
Class:
Protein Ser/Thr
Protein Name:
MARK1
Uniprot Number:
Q9P0L2
Protein Aliases:
MAP/microtubule affinity-regulating kinase 1|PAR1 homolog c|Par-1c|Par1c
Gene Name:
MARK1
Gene ID:
4139
Gene Aliases:
MARK|PAR-1C
Accession Number:
AF154845
Organism:
Human
Construct Details:
2-end; V16E; T20S recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
MARK1 (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 µM KKKVSRSGLYRSPSMPENLNRPR, 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:
100 µM KKKVSRSGLYRSPSMPENLNRPR
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 7.78µM )
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:
MARK1 inhibitors may have therapeutic potential in the treatment of cancers involving colon, liver, prostate and endometrium.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
MARK1 Human CAMK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-651KP
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