Biological Information
Background Information:
Protein serine/threonine kinase Aurora-A (STK6, STK15, BTAK, AIK, ARK1, AURA, Aurora-related kinase 1, Breast-tumor-amplified kinase) is one of a family of serine-threonine kinases that have been strongly linked to chromosome segregation and centrosome functions. There are three isoforms of Aurora kinase: A, B, and C. Molecular mechanism of Aurora-A regulation of G2-M transition is phosphorylation of histone H3. Inhibition of Aurora A may be useful in the treatment of many types of human cancer, including leukemia, colon and breast cancer.
Family:
Kinase
Sub Family:
Other Protein Kinase
Class:
Protein Ser/Thr
Protein Name:
Aurora-A
Uniprot Number:
O14965
Protein Aliases:
protein phosphatase 1, regulatory subunit 47|Aurora-A kinase
Gene Name:
AURKA
Gene ID:
6790
Gene Aliases:
BTAK|AurA|STK7|ARK1|PPP1R47|AIK
Accession Number:
NM_003600
Organism:
Human
Construct Details:
Full length; I31F recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Aurora-A (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 µM LRRASLG (Kemptide), 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:
200 µM LRRASLG (Kemptide)
Tracer:
33P
ATP Concentration:
[ATP]= 10µM (Km= 14µM )
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
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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