AurkA allosteric-IN-1
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA.
For research use only. We do not sell to patients.
- CAS No.: 3035323-39-5
- Formula: C20H16N2O3
- Molecular Weight:332.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Aurora Kinase Isoforms
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Biological Activity
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Aurora A 6.5 μM (IC50, [1]) |
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Cell Line
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Type | Value | Description | References |
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| HeLa | GI50 |
14 μM
Compound: 6h
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Synergistic antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs in presence of PHA-767491 by celltiter-glo assay
Synergistic antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs in presence of PHA-767491 by celltiter-glo assay
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[PMID: 38460487] |
| HeLa | GI50 |
71.7 μM
Compound: 6h
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs in absence of PHA-767491 by celltiter-glo assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs in absence of PHA-767491 by celltiter-glo assay
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[PMID: 38460487] |
AurkA allosteric-IN-1 (100 μM; 48 h) differentially induces cell cycle arrest in different cell types, including lung cancer cell lines and rectal cancer cell lines[1].
AurkA allosteric-IN- 1 (20 μM; 48 h) can downregulate the levels of phospho-histone H3 in cancer cells[1].
AurkA allosteric-IN-1 (25-400 μM; 48 h) exhibits significant anti-cell proliferation on HeLa cells activity, and has a synergistic effect with PHA-767491 (HY-13461), further amplifying its anti-proliferative activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa and Panc-1 cells, Lung cancer cell lines (A549 and H358), and colon cancer cell lines (HT29 and HCT116)
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Concentration:20 μM
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Incubation Time:12, 24, and 48 h
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Result:Arrested cell cycle at G1/S transition in lung cancer cell lines (A549 and H358), and arrested cell cycle at G2/M in colon cancer cell lines (HT29 and HCT116).
Almostly unaffected HeLa and Panc-1 cells.
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Cell Line:HT29 and HCT116 cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:Sharply downregulated the level of phospho-histone H3 (Ser10).
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Cell Line:HeLa cells
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Concentration:25 μM, 50 μM, 100 μM, 200 μM, and 400 μM
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Incubation Time:12, 24, and 48 h; with or without PHA-767491
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Result:With PHA-767491 sensitized HeLa cells, significantly augmented anti-proliferative activity GI50: 71.7 μM to GI50: 14.0 μM by co-treatment of 1.5 μM PHA-76749.
Chemical Information
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CAS No. 3035323-39-5
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Molecular Weight 332.35
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Formula C20H16N2O3
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SMILES
O=C(C1=CC=CC(C2=CC=NC=C2)=C1)NCC3=CC4=C(OCO4)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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