| 产品描述: | Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM |
| 靶点: |
PLK4:0.59 nM (Ki);PLK4 (G95L):497.53 nM (Ki);Aurora A:1239 nM (Ki);Aurora B:5597.14 nM (Ki);AuroraKinase |
| 体外研究: |
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Centrinone-B slightly binds to Aurora A and Aurora B, with Kis of 1239 nM and 5597.14 nM. Centrinone-B (LCR-323) exhibits >1000-fold selectivity for Plk4 over Aurora A/B in vitro and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone-B (LCR-323) (0-200 nM) significantly decreases cell viability of PLK4-centriole conjunction melanoma cell lines except p53 mutant SK-MEL-28, and this effect is via inhibition of PLK4. Inhibition of PLK4 by Centrinone-B (LCR-323) also induces apoptosis in human melanoma cell lines |
| 参考文献: |
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. 2. Denu RA, et al. Centriole Overduplication is the Predominant Mechanism Leading to Centrosome Amplification in Melanoma. Mol Cancer Res. 2018 Jan 12. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.583 ml |
7.915 ml |
15.831 ml |
| 5 mM |
0.317 ml |
1.583 ml |
3.166 ml |
| 10 mM |
0.158 ml |
0.792 ml |
1.583 ml |
| 50 mM |
0.032 ml |
0.158 ml |
0.317 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |