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ZM-447439 Chemical Structure
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Biological Activity
ZM-447439 is a potent and selective Aurora B kinase inhibitor with an IC50 of 50 nM, 1 μM and 250 nM for Aurora B, A and C, respectively. Other kinases such as Cdk1 and PLK1 are not inhibited (up to 10 mM). Cells treated with ZM-447439 progress through interphase, enter mitosis and assemble bipolar spindles but chromosome alignment, segregation and cytokinesis all fail. Mitotic Aurora kinases are essential for accurate chromosome segregation during cell division. Forced overexpression of Aurora kinase results in centrosome amplification and multipolar spindles, causing aneuploidy, a hallmark of cancer. ZM447439 does not interfere with other kinases when used up to 5 µM. ZM447439 dose-dependently inhibited proliferation of all three cell lines (BON, QGP-1 and MIP-101) with IC50 values in the nanomolar to low micromolar range. Moreover, aurora kinase inhibition by ZM447439 potently induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation. [1][2][3]
References on ZM-447439
- [1] Cell Cycle 15 May 2008;7:10, 1473-1479
- [2] The Journal of Cell Biology 2003;161:267–280
- [3] J. Med. Chem 2006;49:955-970
Chemical Information
| Molecular Weight (WM): | 513.59 |
|---|---|
| Formula: | C29H31N5O4 |
| CAS No.: | 331771-20-1 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥103mg/mL |
| Water <1mg/mL | |
| Ethanol ≥48mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Determinants of mitotic catastrophe upon abrogation of the G2 DNA damage checkpoint by UCN-01
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HeLa cells were treated with Nocodazole (100ng/ml) (Lanes 2-4) or Taxol (1µM) (Lanes 6-8) or DMSO (lanes 1, 5) for 16h. The indicated inhibitors were added for 2h (1uM) before harvesting the cells. The p-Aurora-A (T288), B (T232), C (T198) antibody was from Cell Signaling (#2914). MK5108 is an Aurora-A inhibitor. VX680 inhibits all three Aurora kinases. ZM447439 inhibits both Aurora-B and –C kinases, but not Aurora-A kinase. - HeLa cells were treated with Nocodazole (100ng/ml) (Lanes 2-4) or Taxol (1µM) (Lanes 6-8) or DMSO (lanes 1, 5) for 16h. The indicated inhibitors were added for 2h (1uM) before harvesting the cells. The p-Aurora-A (T288), B (T232), C (T198) antibody was from Cell Signaling (#2914). MK5108 is an Aurora-A inhibitor. VX680 inhibits all three Aurora kinases. ZM447439 inhibits both Aurora-B and –C kinases, but not Aurora-A kinase.
Data independently produced by Dr Yuanhong Chen of University of Nebraska ZM-447439 purchased from Selleck
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Click to enlarge
Western blot analysis of Histone and Aurora kinase. 0-10μM ZM447439 was added. - Western blot analysis of Histone and Aurora kinase. 0-10μM ZM447439 was added.
Data independently produced by Dr. Zhang of Tianjin Medical University ZM-447439 purchased from Selleck
- We spoke this morning when I was in a meeting. As feedback I can tell you that we are happy with the ZM-447439 compound and we still have to finalize our studies with the olaparib compound.
Vugt, MUniversity Medical Center Groningen
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| HeLa cells were treated with Nocodazole (100ng/ml) (Lanes 2-4) or Taxol (1µM) (Lanes 6-8) or DMSO (lanes 1, 5) for 16h. The indicated inhibitors were added for 2h (1uM) before harvesting the cells. The p-Aurora-A (T288), B (T232), C (T198) antibody was from Cell Signaling (#2914). MK5108 is an Aurora-A inhibitor. VX680 inhibits all three Aurora kinases. ZM447439 inhibits both Aurora-B and –C kinases, but not Aurora-A kinase. |
Data independently produced by Dr Yuanhong Chen of University of Nebraska
| Western blot analysis of Histone and Aurora kinase. 0-10μM ZM447439 was added. |
Data independently produced by Dr. Zhang of Tianjin Medical University
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