ZM447439

説明

The Aurora kinases have important roles in regulating mitosis and cytokinesis, with Aurora B involved in centromere function as part of the Chromosomal Passenger Complex, with survivin, INCENP, and borealin. ZM 447439 is a selective inhibitor of Aurora B kinase (IC₅₀ = 50 nM), less potently inhibiting Aurora C and A (IC₅₀ = 250 and 1,000 nM, respectively). It has no effect on several other kinases, including Cdk1, Cdk2, Cdk4, Plk1, CHK1, KDR2, and FAK (IC₅₀ > 10 μM). ZM 447439 has been used to study the role of Aurora B in molecular events associated with mitosis and cytokinesis. Moreover, ZM 447439 selectively inhibits proliferating cells rather than non-dividing cells, suggesting its potential in cancer therapy.

化学的特性

Pale Yellow Solid

使用

It is a potent and selective inhibitor of Aurora B kinase. Cells treated with ZM-447439 progress through interphase, enter mitosis and assemble bipolar spindles but chromosome alignment, segregation a nd cytokinesis all fail. It induces apoptosos in Hep2 cancer cells and in acute myeloid leukemia cell lines but its propensity to induce polyploidy does not inevitably result in apoptosis.