Centrinone
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%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Reversible centriole depletion with an inhibitor of Polo-like kinase 4.
Wong et al.
Science, 2015;348:1155 -
Inactivation of PLK4-STIL module prevents self-renewal and triggers p53-dependent differentiation in human pluripotent stem cells.
Renzova et al.
Stem Cell Reports., 2019;11:959 -
TRIM37 controls cancer-specific vulnerability to PLK4 inhibition.
Meitinger et al.
Nature., 2020;
Product Datasheets
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Citations for Centrinone
The citations listed below are publications that use Tocris products. Selected citations for Centrinone include:
7 Citations: Showing 1 - 7
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CPAP insufficiency leads to incomplete centrioles that duplicate but fragment.
Authors: Raj Et al.
J Cell Biol 2022;221
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Oncogenic BRAF induces whole-genome doubling through suppression of cytokinesis.
Authors: Revati Et al.
Nat Commun 2022;13:4109
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PLK4 drives centriole amplification and apical surface area expansion in multiciliated cells.
Authors: Margaret A Et al.
Elife 2022;11
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Mechanical stretch scales centriole number to apical area via Piezo1 in multiciliated cells.
Authors: Brian J Et al.
Elife 2021;10
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Coordination of Zika Virus Infection and Viroplasm Organization by Microtubules and Microtubule-Organizing Centers.
Authors: Hengli Et al.
Cells 2021;10
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PLK4 promotes centriole duplication by phosphorylating STIL to link the procentriole cartwheel to the microtubule wall.
Authors: Tyler Chistopher Et al.
Elife 2019;8
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Spindle-Length-Dependent HURP Localization Allows Centrosomes to Control Kinetochore-Fiber Plus-End Dynamics.
Authors: Patrick Et al.
Curr Biol 2019;29:3563-3578.e6
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