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Hesperadin Aurora B kinase inhibitor

Catalog No.A4118
Size Price Stock Qty
10mM (in 1mL DMSO)
$105.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$90.00
In stock
10mg
$155.00
In stock
50mg
$540.00
In stock
200mg
$1,490.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Hesperadin

Related Biological Data

Hesperadin

Related Biological Data

Hesperadin

Biological Activity

Description Hesperadin is a potent inhibitor of Aurora B with IC50 of 250 nM.
Targets Aurora B (human) TbAUK1        
IC50 250 nM 40 nM        

Protocol

Vitro experiment [1]:

Kinase experiment

Hesperadin is an inhibitor that inserts into the ATP-binding pocket of Aurora A and B. It inhibited Aurora B with IC50 of 250 nM, but has IC50 values in the range of 1.2 μM to >10 μM for Cdk1/cyclin B or Cdk2/cyclin E, respectively. At a concentration of 200 nM, Hesperadin lowered the activity of the immunoprecipitated kinase to the background level.

Cell experiment [2]:

Cell lines

HeLa cells

Preparation method

The solubility of this compound in DMSO is >25.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

50 nM; 2 h

Applications

In HeLa cells, Hesperadin stopped cell proliferating but did not stop growing, and over a 6-d period, the cell diameter increased more than sevenfold (from 20 to 150 μm). The cells acquired enlarged lobed nuclei correlated with polyploidization, reaching a 32C DNA content on day 3. Hesperadin caused defects in mitosis and cytokinesis.

References:

[1]Jetton N1, Rothberg KG, Hubbard JG, Wise J, Li Y, Ball HL, Ruben L. 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 Apr;72(2):442-58. doi: 10.1111/j.1365-2958.2009.06657.x. Epub 2009 Mar 6.

[2]Hauf S1, Cole RW, LaTerra S, Zimmer C, Schnapp G, Walter R, Heckel A, van Meel J, Rieder CL, Peters JM. 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 Apr 28;161(2):281-94. Epub 2003 Apr 21.

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Chemical Properties

Cas No. 422513-13-1 SDF Download SDF
Chemical Name N-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide
Canonical SMILES CCS(=O)(=O)NC1=CC2=C(C=C1)NC(=O)C2=C(C3=CC=CC=C3)NC4=CC=C(C=C4)CN5CCCCC5
Formula C29H32N4O3S M.Wt 516.65
Solubility >25.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Hersperadin is an ATP-competitive small molecule inhibitor of Aurora B kinase, which is one of the three Aurora family kinases involved in the regulation of cell division, with half maximal inhibitory concentration IC50 of 250 nM, where the sulphonamide group of hersperadin inserts into the ATP-pocket in the catalytic cleft of Aurora B kinase and extends into the adjacent hydrophobic pocket. Hersperadin has been found to prevent the phosphorylation of Aurora B, where the Ser-10 phosphorylation of Aurora B in mitosis serves as a biomarker for mitotic progression, with IC50 of 40 nM leading to inhibition of chromosome alignment and segregation.

References:
[1]Jetton N1, Rothberg KG, Hubbard JG, Wise J, Li Y, Ball HL, Ruben L. 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 Apr;72(2):442-58. doi: 10.1111/j.1365-2958.2009.06657.x. Epub 2009 Mar 6.
[2]Hauf S1, Cole RW, LaTerra S, Zimmer C, Schnapp G, Walter R, Heckel A, van Meel J, Rieder CL, Peters JM. 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 Apr 28;161(2):281-94. Epub 2003 Apr 21.