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Submit ReviewCentrinone
Description: High affinity and selective PLK4 inhibitor
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold with the permission of the Ludwig Institute for Cancer Research Ltd
Technical Data for Centrinone
| M. Wt | 633.65 |
| Formula | C26H25F2N7O6S2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Centrinone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.68 | 50 |
Preparing Stock Solutions for Centrinone
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for Centrinone
References for Centrinone
References are publications that support the biological activity of the product.
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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Keywords: Centrinone, Centrinone supplier, High, affinity, selective, PLK4, inhibitors, inhibits, centriole, centrosome, Polo-like, Kinase, Mitosis, ESCs, and, iPSC, 5687, Tocris Bioscience
7 Citations for Centrinone
Citations are publications that use Tocris products. Selected citations for Centrinone include:
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
Do you know of a great paper that uses Centrinone from Tocris? Please let us know.
Reviews for Centrinone
Average Rating: 4 (Based on 1 Review.)
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Nup188 recruitment to the centrosomes.
By
Anonymous on 06/11/2019
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: HeLa
I have used this product in HeLa cells to abolish centrosomes and then track the recruitment kinetics of centriole biogenesis
Literature in this Area
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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.