2. Cell Cycle/DNA Damage Epigenetics
  3. Aurora Kinase
  4. 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.

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AurkA allosteric-IN-1 Chemical Structure

AurkA allosteric-IN-1 Chemical Structure

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AurkA allosteric-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

Aurora A

6.5 μM (IC50, [1])

In Vitro

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.

AurkA allosteric-IN-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HeLa and Panc-1 cells, Lung cancer cell lines (A549 and H358), and colon cancer cell lines (HT29 and HCT116)
Concentration: 20 μM
Incubation Time: 12, 24, and 48 h
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.

Western Blot Analysis[1]

Cell Line: HT29 and HCT116 cells
Concentration: 20 μM
Incubation Time: 48 h
Result: Sharply downregulated the level of phospho-histone H3 (Ser10).

Cell Cytotoxicity Assay[1]

Cell Line: HeLa cells
Concentration: 25 μM, 50 μM, 100 μM, 200 μM, and 400 μM
Incubation Time: 12, 24, and 48 h; with or without PHA-767491
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.
Molecular Weight

332.35

Formula

C20H16N2O3
SMILES

O=C(C1=CC=CC(C2=CC=NC=C2)=C1)NCC3=CC4=C(OCO4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AurkA allosteric-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AurkA allosteric-IN-1Aurora KinaseAllosteric inhibitorAurkAAurora kinaseTPX2Inhibitorinhibitorinhibit

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