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Hesperadin

Cat. No. M2127
Hesperadin Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 65  USD65 In stock
2mg USD 33  USD33 In stock
5mg USD 60  USD60 In stock
10mg USD 90  USD90 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 516.65
Formula C29H32N4O3S
CAS Number 422513-13-1
Purity >99%
Solubility DMSO 73 mg/mL
Storage at -20°C
References

[1] Jetton N, et al. Mol Microbiol. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms.

[2] Sessa F, et al. Mol Cell. Mechanism of Aurora B activation by INCENP and inhibition by hesperadin.

[3] Hauf S, et al. J Cell Biol. The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint.

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Keywords: Hesperadin supplier, Aurora Kinase, inhibitors

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