Centrinone

Research use only, not for human use.

Centrinone (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).

Centrinone (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM). (In Vitro):Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors.

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LCR-263

Cell Cycle/DNA Damage

Aurora Kinase

Aurora A|Aurora B|PLK4|PLK4 G95L

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1798871-30-3

633.65

C26H25F2N7O6S2

>98% (HPLC)

DMSO:31 mg/mL (48.92 mM)

CC1=CC(NC2=NC(SC3=CC=C(S(=O)(CC4=CC=CC([N+]([O-])=O)=C4F)=O)C=C3F)=NC(N5CCOCC5)=C2OC)=NN1

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(-20℃)

With Ice Pack

≥ 2 years