| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥384.00 | 现货 | 1 | |
| 2mg | ¥676.00 | 现货 | 1 | |
| 5mg | ¥1,015.00 | 现货 | 1 | |
| 10mg | ¥1,680.00 | 现货 | 1 | |
| 25mg | ¥2,806.00 | 现货 | 1 | |
| 50mg | ¥3,929.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,415.00 | 现货 | 1 |
Centrinone is an inhibitor of polo-like kinase 4 (Plk4; Ki = 0.16 nM).1 It is greater than 1,100- and 2,800-fold selective for Plk4 over Aurora A and Aurora B kinases, respectively, and a panel of 442 kinases at 100 nM. Centrinone (125 nM) depletes centrosomes and induces apoptosis in HeLa cells.
1.Wong, Y.L., Anzola, J.V., Davis, R.L., et al.Reversible centriole depletion with an inhibitor of polo-like kinase 4Science348(6239)1155-1160(2015)
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Kinase experiment: |
Purified 6xHis-tagged human Plk4 kinase domain is in 20 mM Tris pH 7.5, 100 mM NaCl, 10% glycerol, 1 mM DTT. 2X reaction buffer consists of 50 mM HEPES pH 8.5, 20 mM MgCl2, 1 mM DTT, 0.2 mg/mL BSA, 16 μM ATP, and 200 μM A-A11 substrate. The Plk4 concentration in the final reaction is 2.5-10 nM with a final pH of 8.0. Inhibitors (Centrinone) array in dose response are added from DMSO stocks. Reactions are allowed to proceed for 4-16 hours at 25°C. Detection is performed using ADP-Glo reagent. Luminescence is measured on an plate reader[1]. |
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Cell experiment: |
For each condition, cells are seeded in triplicate into 6-well plates at 50,000 cells/well. 125 nM Centrinone (LCR-263) is added to HeLa cells or 300 nM is added to NIH/3T3 cells. At 24-hour intervals, 3 wells are harvested per condition. Cell counting is performed using a TC10 automated cell counter[1]. |
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References: [1]. Wong YL. et al. Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60. |
