Hesperadin hydrochloride

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Cat.No. 3988 - Hesperadin hydrochloride | C29H32N4O3S.HCl | CAS No. 422513-13-1
Description: Potent Aurora kinase B inhibitor
Chemical Name: N-[2,3-Dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]-ethanesulfonamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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.

Compound Libraries

Hesperadin hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 553.12
Formula C29H32N4O3S.HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 422513-13-1
PubChem ID 76968689
InChI Key XMYLEXZLFZAOQN-LXCLTORNSA-N
Smiles O=C3/C(C2=CC(NS(CC)(=O)=O)=CC=C2N3)=C(C4=CC=CC=C4)\NC1=CC=C(CN5CCCCC5)C=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.31 100
ethanol 27.66 50

Preparing Stock Solutions

The following data is based on the product molecular weight 553.12. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.81 mL 9.04 mL 18.08 mL
5 mM 0.36 mL 1.81 mL 3.62 mL
10 mM 0.18 mL 0.9 mL 1.81 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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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Keywords: aurora B kinase inhibitors inhibits ATP-competitive Aurora Kinases

Citations for Hesperadin hydrochloride

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for Hesperadin hydrochloride

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