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说明： High affinity and selective PLK4 inhibitor
化学名： 2-[[2-Fluoro-4-[[(2-fluoro-3-nitrophenyl)methyl]sulfonyl]phenyl]thio]-5-methoxy-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-morpholinyl)-4-pyrimidinamine
纯度： ≥98% (HPLC)
生物活性 for Centrinone
Centrinone is a high affinity and selective PLK4 inhibitor (Ki = 0.16 nM). Exhibits >1000-fold selectivity for PLK4 over Aurora A and Aurora B. Depletes centriole and centrosome levels in vitro. Induces cell cycle arrest in normal human cell lines in a p53-dependent manner. Decreases expression of pluripotency markers and induces differentiation in pluripotent stem cells.
许可信息
Sold with the permission of the Ludwig Institute for Cancer Research Ltd
技术数据 for Centrinone
| 分子量 | 633.65 |
| 公式 | C26H25F2N7O6S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1798871-30-3 |
| PubChem ID | 91801159 |
| InChI Key | HHJSKDRCUMVWKF-UHFFFAOYSA-N |
| Smiles | FC1=C([N+]([O-])=O)C=CC=C1CS(C2=CC=C(SC3=NC(N4CCOCC4)=C(OC)C(NC5=NNC(C)=C5)=N3)C(F)=C2)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Centrinone
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.68 | 50 |
制备储备液 for Centrinone
以下数据基于产品分子量 633.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.16 mL | 15.78 mL | 31.56 mL |
| 2.5 mM | 0.63 mL | 3.16 mL | 6.31 mL |
| 5 mM | 0.32 mL | 1.58 mL | 3.16 mL |
| 25 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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产品说明书 for Centrinone
参考文献 for Centrinone
参考文献是支持产品生物活性的出版物。
Wong et al (2015) Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science 348 1155 PMID: 25931445
Renzova et al (2019) Inactivation of PLK4-STIL module prevents self-renewal and triggers p53-dependent differentiation in human pluripotent stem cells. Stem Cell Reports. 11 959 PMID: 30197118
Meitinger et al (2020) TRIM37 controls cancer-specific vulnerability to PLK4 inhibition. Nature. PMID: 32908304
If you know of a relevant reference for Centrinone, please let us know.
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关键词: Centrinone, Centrinone supplier, High, affinity, selective, PLK4, inhibitors, inhibits, centriole, centrosome, Polo-like, Kinase, Mitosis, ESCs, and, iPSC, 5687, Tocris Bioscience
7 篇 Centrinone 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Centrinone 的部分引用包括：
Tyler Chistopher et al (2019) PLK4 promotes centriole duplication by phosphorylating STIL to link the procentriole cartwheel to the microtubule wall. Elife 8 PMID: 31115335
Patrick et al (2019) Spindle-Length-Dependent HURP Localization Allows Centrosomes to Control Kinetochore-Fiber Plus-End Dynamics. Curr Biol 29 3563-3578.e6 PMID: 31668617
Revati et al (2022) Oncogenic BRAF induces whole-genome doubling through suppression of cytokinesis. Nat Commun 13 4109 PMID: 35840569
Margaret A et al (2022) PLK4 drives centriole amplification and apical surface area expansion in multiciliated cells. Elife 11 PMID: 35969030
Raj et al (2022) CPAP insufficiency leads to incomplete centrioles that duplicate but fragment. J Cell Biol 221 PMID: 35404385
Brian J et al (2021) Mechanical stretch scales centriole number to apical area via Piezo1 in multiciliated cells. Elife 10 PMID: 34184636
Hengli et al (2021) Coordination of Zika Virus Infection and Viroplasm Organization by Microtubules and Microtubule-Organizing Centers. Cells 10 PMID: 34943843
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Centrinone 的评论
平均评分: 4 (Based on 1 Review.)
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Nup188 recruitment to the centrosomes.
By
Anonymous on 06/11/2019
分析类型： In Vivo
种属： Mouse
细胞系/组织： HeLa
I have used this product in HeLa cells to abolish centrosomes and then track the recruitment kinetics of centriole biogenesis
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.