Cat. No. Name Size Price Add Cart
KI0002Hesperadin5 mg$272
Hesperadin10 mg$512
Hesperadin50 mg$1552
Hesperadin200 mg$3952

Chemical Characteristic

Product NameHesperadin
CAS No.422513-13-1
Molecular Weight 516.65
FormulaC29H32N4O3S
Chemical NameN-[2,3-Dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]ethanesulfonamide
SmilesC(C)S(=O)(=O)Nc1cc2/C(=C(/Nc3ccc(cc3)CN3CCCCC3)\c3ccccc3)/C(=O)Nc2cc1
Chemical Structure

Biological activities

Hesperadin is an indolinone inhibitor of human Aurora B with an IC50 of 250 nM. Hesperadin also potently inhibits Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with an IC50 of 40 nM. Hesperadin (1 µM) markedly reduces the activity of six kinases (AMPK, Lck, MKK1, MAPKAP-K1, CHK1, and PHK). Besides, Hesperadin half-maximally inhibits Cdk1/cyclin B and Cdk2/cyclinE at the concentrations of 2.8 and ??10 µM, respectively. Hesperadin (100 nM) causes defects in mitosis and cytokinesis in HeLa cells. Hesperadin (20-100 nM) induces polyploidization and loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Hesperadin-treated (50 nM) HeLa cells also show alignment and segregation defects, but sister chromatid separation is intact. Hesperadin-treated (500 nM) PtK cells show a higher frequency of syntelic attachments during prometaphase than control-treated cells. Hesperadin (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol in HeLa cells.[1] Hesperadin inhibits the TbAUK1-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner. Hesperadin is effective at inhibiting growth of bloodstream forms (BF) cultures with IC50 of 50 nM, while the inhibition of procyclic forms (PF) growth requires approximately 11-fold more hesperadin, with an IC50 of 550 nM.[2] On the acute lung inflammation model induced by lipopolysaccharide (LPS) in vivo, hesperidin (200 mg/kg oral administration) downregulates the LPS-induced expression of TNF-α, IL-1β, IL-6, KC, MIP-2, MCP-1, and IL-12 and also enhances the production of IL-4, IL-10. In addition, hesperidin significantly decreases total leukocyte counts, nitric oxide production and iNOS expression.[3]

Protocols

Hesperidin is suspended in saline (1 mM).[3]

References

[1] Hauf S, et al. 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. 2003, 161(2): 281-294.
[2] Jetton N, et al. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol Microbiol. 2009, 72(2): 442-458.
[3] Yeh CC, et al. The immunomodulation of endotoxin-induced acute lung injury by hesperidin in vivo and in vitro. Life Sci. 2007, 80(20): 1821-1831.

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