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    Hesperadin
    Hesperadin

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0361
    CAS #: 422513-13-1Purity ≥98%

    Description: Hesperadin is a novel, potent and ATP-competitive inhibitor of human aurora B kinase with potential antitumor activity. It inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo. Hersperadin shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.  

    References: J Cell Biol. 2003 Apr 28;161(2):281-94; Mol Microbiol. 2009 Apr;72(2):442-58.

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    • 香港大学
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    Molecular Weight (MW)516.65
    FormulaC29H32N4O3S
    CAS No.422513-13-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 103 mg/mL (199.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    Synonyms

    Hesperadine; Hesperadin; 

    Hesperadine; (Z)-N-(2-oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulfonamide

    InChi Key: GLDSKRNGVVYJAB-DQSJHHFOSA-N

    InChi Code: InChI=1S/C29H32N4O3S/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34)/b28-27-

    SMILES Code: CCS(=O)(NC1=CC2=C(NC(/C2=C(C3=CC=CC=C3)\NC4=CC=C(CN5CCCCC5)C=C4)=O)C=C1)=O 


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    In Vitro

    In vitro activity: Hesperadin 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. In contrast, only 20-100 nM of Hesperadin is sufficient to induce the loss of mitotic histone H3-Ser10 phosphorylation in HeLa cells. Hesperadin treatment causes defects in mitosis and cytokinesis, leading to stoppage of proliferation of HeLa cells and polyploidization, which can be specifically ascribed to the inhibition of Aurora B function during the process of chromosome attachment. Hesperadin (100 nM) quickly overrides the mitotic arrest induced by taxol or monastrol but not by nocodazole. Hesperadin and nocodazole treatment in HeLa cells abolishes kinetochore localization of BubR1 and diminishes the intensity of Bub1 at kinetochores, suggesting that Aurora B function is required for efficient kinetochore recruitment of BubR1 and Bub1, which in turn might be necessary for prolonged checkpoint signaling. Hesperadin prevents the phosphorylation of recombinant trypanosome histone H3 by the T. brucei Aurora kinase-1 (TbAUK1) from pathogenic Trypanosoma brucei with IC50 of 40 nM in vitro kinase assays. Hesperadin significantly inhibits cell growth of cultured infectious bloodstream forms (BF) with IC50 of 48 nM, and only weakly inhibits cell growth of insect stage procyclic forms (PF) with IC50 of 550 nM.


    Kinase Assay: For the Aurora B kinase assay, HeLa cells are lysed in a buffer containing 50 mM NaCl. The whole cell extract is spun at 13,000 rpm for 20 minutes at 4 °C using a table top centrifuge. The pellet obtained from 200 mg of whole cell extract is extracted again in 15 mL lysis buffer containing 250 mM NaCl in order to obtain active Aurora B kinase from mitotic chromatin. The low speed supernatant of the latter extract is used for immunoprecipitation. Monoclonal mouse anti–AIM-1, or mouse anti-HA, is coupled to GammaBind Plus Sepharose, and beads are rotated over-end in the extract for 90 minutes at 4 °C. Beads are washed, aliquoted, and washed in kinase buffer (20 mM Tris, pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, 10 mM NaF). The kinase assay is performed with 10 μL beads in 20 μL kinase buffer containing 5 μg histone H3, 10 μM ATP, 2.5 μCi [γ-32P]ATP, and different concentrations of Hesperadin for 20 minutes at 37 °C. SDS sample buffer is added, and samples are boiled and resolved by SDS-PAGE. The gel is dried, and the radioactive signal is detected by PhosphorImager analysis. The data is analyzed using ImageQuant software.


    Cell Assay: Cells (HeLa cells and PtK1 cells) are exposed to different concentrations of Hesperadin for 24 and 48 hours. At indicated time points, methanol-fixed cell samples are washed with PBS and subsequently stained in PI buffer (50 μg/mL propidium iodide, 10 mM Tris, pH 7.5, 5 mM MgCl2, 200 μg/mL RNase A) for 20-40 minutes at 37 °C. The DNA content is determined by flow cytometry.

    In VivoHA-680632 (15–60 mg/kg) inhibits tumor growth in mice xenografts models of HL60, A2780, and HCT116 cells, by reducing tumor cell proliferation and increasing apoptosis. PHA-680632 (45 mg/kg) suppresses growth of activated ras-driven mammary tumors in mouse mammary tumor virus v-Ha-ras transgenic mice and results in complete tumor stabilization and partial regression.
    Animal modelMice (female athymic nude) xenografts models of p53−/− HCT116 cells
    Formulation & DosageDissolved in 20% Tween-80 in 5% glucose solution; 40 mg/kg; i.p. injection BID
    References

    J Cell Biol. 2003 Apr 28;161(2):281-94; Mol Microbiol. 2009 Apr;72(2):442-58.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Hesperadin

    Hesperadin

    Hesperadin

    In vitro kinase assay of TbAUK1. Mol Microbiol. 2009 Apr; 72(2): 442–458.


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