Biological Information
Background Information:
Aurora family of kinases, contained at least three proteins (Aurora A, B and C), phosphorylate histone H3 and provide a direct path to the nucleosome. Aurora-B (AURAKB, AIK2, AIM1, ARK2, STK12) is needed for metaphase alignment of chromosomes, sister chromatid separation and cytokinesis. Overexpression of Aurora-B is found in several types of cancer and causes dramatic increases in genomic instability.
Family:
Kinase
Sub Family:
Other Protein Kinase
Class:
Protein Ser/Thr
Protein Name:
Aurora-B
Uniprot Number:
Q96GD4
Protein Aliases:
aurora-B|aurora-1|protein phosphatase 1, regulatory subunit 48
Gene Name:
AURKB
Gene ID:
9212
Gene Aliases:
Aik2|IPL1|AurB|AIM-1|ARK2|STK5|PPP1R48
Accession Number:
NM_004217
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:
Human recombinant protein kinase Aurora-B expressed in insect S21 cells is used. Test compound is preincubated with 4.2 μg/ml enzyme‡ in modified MOPS buffer pH 7.2 for 15 minutes at 37°C. The reaction is initiated by addition of 100 μM kemptide, 10 μM ATP containing 0.05 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]Kemptide. Compounds are screened at 10 μM.
Substrate:
100 µM Kemptide
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:
10
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Adverse / Beneficial Action:
Inhibition of Aurora-B may be useful in the treatment of several solid tumors including breast, ovary, prostate, pancreas and colorectal cancer.
Additional Information
Brand:
Panlabs
Testing Location:
Taiwan - Taipei