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.
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The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint.
Hauf, S et al.
J Cell Biol;161(2):281-94.
The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms.
Jetton et al.
Mechanism of Aurora B activation by INCENP and inhibition by Hesperadin.
Sessa et al.