S84011 |
Centrinone |
源叶(MedMol) | ≥98%(HPLC) |
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- 产品描述: Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
- 靶点: PLK4:0.16 nM (Ki);PLK4 (G95L):68.57 nM (Ki);Aurora A:171 nM (Ki);Aurora B:436.76 nM (Ki);PLK; AuroraKinase
- 体外研究:
Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors.
- 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.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.578 ml 7.891 ml 15.782 ml 5 mM 0.316 ml 1.578 ml 3.156 ml 10 mM 0.158 ml 0.789 ml 1.578 ml 50 mM 0.032 ml 0.158 ml 0.316 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)