Name: Hesperadin
Price: 268.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
    
    [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.
- Properties
  - Alternative Name
    
    N-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide
    
    CAS Number
    
    422513-13-1
    
    Molecular Formula
    
    C29H32N4O3S
    
    Molecular Weight
    
    516.65
    
    Appearance
    
    A solid
    
    Purity
    
    98.29%
    
    Solubility
    
    ≥25.85 mg/mL in DMSO; insoluble in H2O; ≥2.31 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Maik Schuler, Lindsay Tomlinson, et al. "Experiments in the EpiDerm 3D Skin In Vitro Model and Minipigs In Vivo Indicate Comparatively Lower In Vivo Skin Sensitivity of Topically Applied Aneugenic Compounds." Toxicol Sci. 2021 Feb 26;180(1):103-121. PMID:33481035
    2. Kaisari S, Shomer P, et al. "Role of Polo-like kinase 1 in the regulation of the action of p31(comet) in the disassembly of mitotic checkpoint complexes." Proc Natl Acad Sci U S A. 2019 Jun 11;116(24):11725-11730. PMID:31118282
    3. Manuel Saldivia, Srinivasa P.S. Rao, et al. "Targeting the trypanosome kinetochore with CLK1 protein kinase inhibitors." bioRxiv. 2019 April 24.

Hesperadin

Hesperadin

Background

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