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
Biological ActivityCentrinone 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.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Reversible centriole depletion with an inhibitor of Polo-like kinase 4.
Wong et al.
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.
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