S84012 |
Centrinone-B |
源叶(MedMol) | 98% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)