Drug intelligence / Profile preview

hesperadin

Development stage
Preclinical
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Intravenous
01

Overview

Hesperadin is a potent and selective small molecule inhibitor of **Aurora B kinase**. Originally developed by researchers at **Boehringer Ingelheim**, it serves as a critical tool compound in cell biology for investigating the mechanisms of mitosis. By inhibiting Aurora B, hesperadin interferes with the attachment of spindle microtubules to kinetochores, preventing proper chromosome alignment and segregation. This disruption triggers the spindle assembly checkpoint (SAC) or leads to polyploidy and subsequent apoptosis in cancer cells. In preclinical studies, hesperadin has shown efficacy against **T-cell acute lymphoblastic leukemia (T-ALL)**, particularly when combined with HDAC inhibitors like chidamide, by promoting the degradation of the **c-MYC** oncoprotein and inducing G2/M cell cycle arrest.

02

Targets

AURKB (Aurora kinase B)AMPK (Adenosine monophosphate–activated protein kinase)CHEK1 (Checkpoint kinase 1)RSK (RSK family)PHKA2 (Phosphorylase Kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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