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  3. Hesperadin

Hesperadin 

Cat. No.: HY-12054 Purity: >98.0%
Handling Instructions

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM.

For research use only. We do not sell to patients.

Hesperadin Chemical Structure

Hesperadin Chemical Structure

CAS No. : 422513-13-1

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10 mM * 1  mL in DMSO USD 68 In-stock
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10 mg USD 90 In-stock
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50 mg USD 250 In-stock
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100 mg USD 450 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Hesperadin:

Top Publications Citing Use of Products

Publications Citing Use of MCE Hesperadin

    Hesperadin purchased from MCE. Usage Cited in: Behav Neurol. 2020 Feb 3;2020:2476861.

    Administration of hesperadin influences endogenous expression of MST4, pAKT, AKT, and LC3 12 h following ICH. Representative western blot bands for MST4, pAKT, AKT, and LC3 expression in sham and ICH mice 12 h following ICH.

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    Description

    Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM[1].

    IC50 & Target[1]

    Aurora B

    250 nM (IC50)

    In Vitro

    Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM[1].
    Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures[1].
    Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1[1].

    Cell Viability Assay[1]

    Cell Line: M110 cells
    Concentration: 0.01, 0.1, 1, 10 μM
    Incubation Time: 24 hours or 48 hours
    Result: Inhibiting growth of BF cultures with IC50 of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with IC50 of 550 nM.

    Cell Cycle Analysis[1]

    Cell Line: M110 cells
    Concentration: 100, 200 nM
    Incubation Time: 24, 48, 72 hours
    Result: Had a strong effect on cell growth and mitotic progression at 100-200 nM.
    In Vivo

    Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with temozolomide (TMZ)[2].

    Animal Model: 6-week-old female nude mice injected GBM cells[2]
    Dosage: 20 mg/kg/d
    Administration: I.v. injection
    Result: Increased the survival of xenograft mice models.
    Molecular Weight

    516.65

    Formula

    C₂₉H₃₂N₄O₃S

    CAS No.

    422513-13-1

    SMILES

    O=C1NC2=CC=C(C=C2/C1=C(NC3=CC=C(C=C3)CN4CCCCC4)\C5=CC=CC=C5)NS(CC)(=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (193.55 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9355 mL 9.6777 mL 19.3555 mL
    5 mM 0.3871 mL 1.9355 mL 3.8711 mL
    10 mM 0.1936 mL 0.9678 mL 1.9355 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    HesperadinAurora KinaseAutophagyInfluenza VirusParasiteAuroraABbloodstreamprocyclicformsBFPFInhibitorinhibitorinhibit

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