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Hesperadin

Cat. No. M2127

Hesperadin Structure
Size Price Availability Quantity
10mg USD 155 In stock
50mg USD 540 In stock
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Quality Control
Biological Activity

Hesperadin is an inhibitor of human Aurora B, prevented the phosphorylation of substrate with IC50 of 40 nM. Hesperadin significantly inhibits cell growth of cultured bloodstream forms with IC50 of 50 nM. Hesperadin also 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. Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Molecular models predicted high-affinity binding of Hesperadin to both conserved and novel sites in TbAUK1. Hesperadin treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 516.65
Formula C29H32N4O3S
CAS Number 422513-13-1
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
References

The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms.
Jetton N, et al. Mol Microbiol. 2009 Apr;72(2):442-58. PMID: 19320832.

Mechanism of Aurora B activation by INCENP and inhibition by hesperadin.
Sessa F, et al. Mol Cell. 2005 Apr 29;18(3):379-91. PMID: 15866179.

The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint.
Hauf S, et al. J Cell Biol. 2003 Apr 28;161(2):281-94. PMID: 12707311.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Hesperadin supplier, Aurora Kinase, inhibitors

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