ZM 447439 is a novel, potent and selective inhibitor of Aurora kinase, a family of serine/threonine kinases essential for accurate chromosome segregation during cell division, that inhibits the activity of purified recombinant Aurora A and Aurora B proteins in vitro with 50% inhibition concentration IC50 values of 110 nM and 130 nM respectively and hence inhibits phosphorylation of histone H3 on serine 10. Being specifically for Aurora kinases, ZM 447439 barely inhibits the majority of other protein kinases (IC50 > 10 μM), such as CDK1/2/4, IKK1/2, PLK1, CHK1, cFLT2, KDR2, FAK and Zap-70, except for MEK1, SRC and LCK (IC50 values of 1.79 μM, 1.03 and 0.88 μM respectively μM).
Reference
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