Hesperadin hydrochloride

Biological Activity

Hesperadin hydrochloride is an 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. Inhibits replication of influenza A and B viral strains (IC₅₀ values range from 0.22 μM to 1.8 μM, dependant on strain), by inhibiting viral RNA transcription and translation

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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.
2. 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.
   Mol.Microbiol., 2009;72:442
3. Mechanism of Aurora B activation by INCENP and inhibition by Hesperadin.
   Sessa et al.
   Mol.Cell., 2005;18:379
4. Chemical genomics approach leads to the identification of hesperadin, an aurora B kinase inhibitor, as a broad-spectrum influenza antiviral.
   Hu et al.
   Int.J.Mol.Sci., 2017;18:1929

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