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ZM447439 is an Aurora kinase B inhibitor, suppresses the growth of cervical cancer SiHa cells and enhances the chemosensitivity to cisplatin. Aurora family kinases play roles in several mitotic processes, including the G2/M transition, mitotic spindle organization, chromosome segregation, and cytokinesis. ZM447439 has dramatic effects on chromosome morphology and spindle dynamics. ZM-447439 can reduce the number of SiHa cells, increase the volume of cells and lead to apoptosis. The growth of SiHa cells treated with ZM447439 was inhibited in dose- and time-dependent manners. ZM447439 significantly inhibited the expression of Aurora-B and H3-P protein (P < 0.05). ZM-447439 selectively over a range of other kinases such as Cdk1 and PLK1 (up to 10mM). Additionally, aurora kinase inhibition by ZM447439 potently induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation.
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Source | Concordia University (2015). Figure 9. ZM447439 (Abmole Bioscience) |
| Method | Inhibit Aurora B kinase | |
| Cell Lines | MDCK cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | 20-‐40 min | |
| Results | Upon treating MDCK cells with an 35 Aurora B inhibitor, ZM447439, we found that the number asymmetrically ingressing cells was not statistically changed in comparison to control cells |
| Cell Experiment | |
|---|---|
| Cell lines | MCF7 cells |
| Preparation method | Cell cycle analysis and cloning assays. DNA content and mitotic index measurements and synchronization of TA-HeLa cells at G1/S using a double thymidine block were done as described previously (Taylor and McKeon, 1997). To determine cloning efficiency, MCF7 cells were plated in phenol red free DME plus 5% stripped serum (HyClone), and were then treated with or without the anti-estrogen ICI 182780 at 1 μM for 48 h. ZM447439 was then added at the indicated concentrations for 72 h. The cells were harvested, washed, and ∼400 cells plated in each well of a 6-well plate in complete media without ZM447439. After 10 d, the colonies were fixed, stained with crystal violet, and counted. The cloning efficiency represents the number of colonies on ZM447439-treated plates compared with DMSO-treated controls. |
| Concentrations | 0~5 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | MOLM13 cells in murine xenograft model |
| Formulation | 3 M Tris, pH 9.0, at a concentration of 2.5 mg/mL |
| Dosages | 5 mg/kg 4 times a week for 2 weeks |
| Administration | intraperitoneal injection |
| Molecular Weight | 513.59 |
| Formula | C29H31N5O4 |
| CAS Number | 331771-20-1 |
| Solubility (25°C) | DMSO 53 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Aurora Kinase Products |
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AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora B and Aurora A respectively. |
| CCT-129202
CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. |
| CYC116
CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. |
| ENMD-2076
ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor. |
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