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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)
Citations (7)
Reviews (1)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

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

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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

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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.