1. Cell Cycle/DNA Damage Epigenetics Autophagy Anti-infection
  2. Aurora Kinase Autophagy Influenza Virus Parasite
  3. Hesperadin

Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

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Hesperadin Chemical Structure

Hesperadin Chemical Structure

CAS No. : 422513-13-1

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Hesperadin:

Top Publications Citing Use of Products

    Hesperadin purchased from MedChemExpress. Usage Cited in: Behav Neurol. 2020 Feb 3;2020:2476861.  [Abstract]

    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.
    • Biological Activity

    • Purity & Documentation

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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. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral[1][2][3].

    IC50 & Target[1]

    Trypanosoma

     

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (193.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9355 mL 9.6777 mL 19.3555 mL 48.3887 mL
    5 mM 0.3871 mL 1.9355 mL 3.8711 mL 9.6777 mL
    10 mM 0.1936 mL 0.9678 mL 1.9355 mL 4.8389 mL
    15 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2259 mL
    20 mM 0.0968 mL 0.4839 mL 0.9678 mL 2.4194 mL
    25 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9355 mL
    30 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
    40 mM 0.0484 mL 0.2419 mL 0.4839 mL 1.2097 mL
    50 mM 0.0387 mL 0.1936 mL 0.3871 mL 0.9678 mL
    60 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8065 mL
    80 mM 0.0242 mL 0.1210 mL 0.2419 mL 0.6049 mL
    100 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4839 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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