包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Kinase experiment | Hesperadin is an inhibitor that inserts into the ATP-binding pocket of Aurora A and B. It inhibited Aurora B with IC50 of 250 nM, but has IC50 values in the range of 1.2 μM to >10 μM for Cdk1/cyclin B or Cdk2/cyclin E, respectively. At a concentration of 200 nM, Hesperadin lowered the activity of the immunoprecipitated kinase to the background level. |
Cell lines | HeLa cells |
Preparation method | The solubility of this compound in DMSO is >25.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 50 nM; 2 h |
Applications | In HeLa cells, Hesperadin stopped cell proliferating but did not stop growing, and over a 6-d period, the cell diameter increased more than sevenfold (from 20 to 150 μm). The cells acquired enlarged lobed nuclei correlated with polyploidization, reaching a 32C DNA content on day 3. Hesperadin caused defects in mitosis and cytokinesis. |
产品描述 | Hersperadin is an ATP-competitive small molecule inhibitor of Aurora B kinase, which is one of the three Aurora family kinases involved in the regulation of cell division, with half maximal inhibitory concentration IC50 of 250 nM, where the sulphonamide group of hersperadin inserts into the ATP-pocket in the catalytic cleft of Aurora B kinase and extends into the adjacent hydrophobic pocket. Hersperadin has been found to prevent the phosphorylation of Aurora B, where the Ser-10 phosphorylation of Aurora B in mitosis serves as a biomarker for mitotic progression, with IC50 of 40 nM leading to inhibition of chromosome alignment and segregation. References: |