Drug intelligence / Profile preview

centrinone-B

Development stage
Preclinical
Lead developer
University of California, San Francisco
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Centrinone-B is a potent and selective small-molecule inhibitor of Polo-like kinase 4 (PLK4), the master regulator of centriole duplication in human cells. Developed as a chemical probe, centrinone-B is used to induce the reversible depletion of centrosomes, leading to cell cycle arrest and apoptosis in certain cancer types. In preclinical research, particularly in melanoma, centrinone-B has demonstrated significant anti-proliferative effects by inducing G0/G1 phase arrest and programmed cell death. It is widely utilized in cell biology to study centrosome function and is being evaluated as a potential therapeutic lead for neoplasms where PLK4 is overexpressed. Centrinone-B is an analog of the original centrinone compound, often preferred in specific research contexts due to its distinct pharmacological and selectivity profile.

02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)PLK4 (Polo-like kinase 4)

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