1. Epigenetics
    Cell Cycle/DNA Damage
    Autophagy
  2. Aurora Kinase
    Autophagy

Hesperadin 

Cat. No.: HY-12054 Purity: 99.67%
Data Sheet SDS Handling Instructions

Hesperadin is a ATP-competitive inhibitor of Aurora B kinase with IC50 of 250 nM.

For research use only. We do not sell to patients.
Hesperadin Chemical Structure

Hesperadin Chemical Structure

CAS No. : 422513-13-1

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10 mM * 1 mL in DMSO $102 In-stock
5 mg $90 In-stock
10 mg $155 In-stock
50 mg $540 In-stock
100 mg $850 In-stock
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  • Biological Activity

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  • Technical Information

  • Purity & Documentation

  • References

Description

Hesperadin is a ATP-competitive inhibitor of Aurora B kinase with IC50 of 250 nM. IC50 Value: 250 nM Target: Aurora B in vitro: Hesperadin prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. Hesperadin significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM. Hesperadin inhibits the ability of immunoprecipitated Aurora B to phosphorylate histone H3 with IC50 of 250 nM and markedly reduces the activity of other kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK) at a concentration of 1 μM. In contrast, only 20-100 nM of Hesperadin is sufficient to induce the loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Hesperadin treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. Hesperadin (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol but not by nocodazole. Hesperadin and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. in vivo:

References
Molecular Weight

516.65

Formula

C₂₉H₃₂N₄O₃S

CAS No.

422513-13-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Hesperadin
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HY-12054
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