A multi-kinase inhibitor
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ATP-competitive inhibitor of Aurora B kinase (IC50 = 250 nM). Prevents chromosome alignment and segregation; also induces polyploidy and prevents histone H3-Ser10 phosphorylation. Overrides the spindle assembly checkpoint and induces mitotic exit in monastrol- and taxol-treated HeLa cells.
Hauf et al (2003) The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. J.Cell.Biol. 161 281 PMID:12707311 |Jetton et al (2009) The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol.Microbiol. 72 442 PMID:19320832 |Sessa et al (2005) Mechanism of Aurora B activation by INCENP and inhibition by Hesperadin. Mol.Cell. 18 379 PMID:15866179
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