Molecular Weight(MW): 513.59
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
Cited by 12 Publications
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p31comet depletion delays MCC disassembly even with the proteasome inhibited. (A) FACS analysis of HeLa Tet-on cells transfected with control or p31comet siRNA and then treated with Taxol followed by Aurora B inhibition with ZM447439. The percentage of mitotic cells (cells that have 4N DNA content and are MPM2 positive) is shown for each sample.
Mol Biol Cell 2011 22, 4227-35. ZM 447439 purchased from Selleck.
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 (1 µM) 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.
Dr. Yuanhong Chen of University of Nebraska. ZM 447439 purchased from Selleck.
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|Description||ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.|
|Features||An Aurora selective ATP-competitive inhibitor.|
In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM.  Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle.  In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle.  A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin. 
In vitro kinase assays :Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen.
|In vitro||DMSO||103 mg/mL (200.54 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
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