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Submit ReviewHesperadin hydrochloride
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)
Biological Activity for Hesperadin hydrochloride
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
Compound Libraries for Hesperadin hydrochloride
Hesperadin hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for Hesperadin hydrochloride
| M. Wt | 553.12 |
| Formula | C29H32N4O3S.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Hesperadin hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 55.31 | 100 | |
| ethanol | 27.66 | 50 |
Preparing Stock Solutions for Hesperadin hydrochloride
The following data is based on the product molecular weight 553.12. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for Hesperadin hydrochloride
References for Hesperadin hydrochloride
References are publications that support the biological activity of the product.
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
Hu et al (2017) Chemical genomics approach leads to the identification of hesperadin, an aurora B kinase inhibitor, as a broad-spectrum influenza antiviral. Int.J.Mol.Sci. 18 1929 PMID: 28885544
If you know of a relevant reference for Hesperadin hydrochloride, please let us know.
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Keywords: Hesperadin hydrochloride, Hesperadin hydrochloride supplier, aurora, B, kinase, inhibitors, inhibits, ATP-competitive, 422513-13-1, antiviral, influenza, virus, Aurora, Kinases, Influenza, Viruses, 3988, Tocris Bioscience
2 Citations for Hesperadin hydrochloride
Citations are publications that use Tocris products. Selected citations for Hesperadin hydrochloride include:
Judith et al (2019) DGAT2 partially compensates for lipid-induced ER stress in human DGAT1-deficient intestinal stem cells. J Lipid Res 60 1787-1800 PMID: 31315900
Damarys et al (2020) Histone variant H3.3 residue S31 is essential for Xenopus gastrulation regardless of the deposition pathway. Nat Commun 11 1256 PMID: 32152320
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Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
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. 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.