1. Thiostrepton

Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation.

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Thiostrepton Chemical Structure

Thiostrepton Chemical Structure

CAS No. : 1393-48-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Thiostrepton purchased from MedChemExpress. Usage Cited in: Environ Pollut. 2018 Aug 17;242(Pt B):1535-1545.  [Abstract]

    RWPE-1 cells are pretreated with Thiostrepton at 5 µM for 1 h and subsequently exposed to MC-LR (100 nM) for 48 h; expressions of FOXM1, β-catenin, CyclinD1 and PSA are detected by western blotting. Expression levels of FOXM1 and β-catenin in the nuclei of RWPE-1 cells are examined by western blotting assay.

    Thiostrepton purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Oct;37(41):5520-5533.  [Abstract]

    Proliferation of CLL cells with lentivirus mediated FoxM1 knockdown or incubation of 1 μM FoxM1 inhibitor Thiostrepton treatment reduces significantly relative to the control group (p<0.05).
    • Biological Activity

    • Purity & Documentation

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    Description

    Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation[1].

    In Vitro

    Thiostrepton (0.01-1000 μM; 48 hours) suppresses cell viability in A2780 and HEC-1A[2].

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

    Cell Viability Assay[2]

    Cell Line: A2780 and HEC-1A cells
    Concentration: 0.01, 0.1, 1, 10, 100, 1000 μM
    Incubation Time: 48 hours
    Result: The IC50s are 1.10 μM in A2780 and 2.22 μM in HEC-1A, respectively.
    In Vivo

    Thiostrepton (i.p.; 17 mg/kg) reduces the tumorigenicity of Ewing's sarcoma (EWS) cells. Tumor volumes in control mice have increased ~6-fold from the initiation of treatment, while their Thiostrepton-treated counterparts increase only ~1.7-fold, exhibiting a ~3.5-fold reduction, relative to controls[3].

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

    Animal Model: Athymic (BALB/c nu/nu) nude mice bearing A4573 cells[3]
    Dosage: 17 mg/kg
    Administration: Administered i.p.
    Result: Treatment inhibited the growth of EWS-derived tumors in vivo.
    Molecular Weight

    1664.89

    Formula

    C72H85N19O18S5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@H](NC(C(NC([C@@H](NC(C(NC(C=C1)C2([H])O)[C@@H](C)CC)=O)C)=O)=C)=O)C)N[C@](C3=NC(C(NC(C(N/C(C4=N[C@]5([H])CS4)=C\C)=O)[C@H](O)C)=O)=CS3)(CCC(C6=NC(C(NC(C(NC(C(N)=O)=C)=O)=C)=O)=CS6)=N7)[C@@]7([H])C8=CSC([C@@]([C@H](OC(C9=CC([C@@H](O)C)=C1C2=N9)=O)C)([H])NC(C%10=CSC([C@](NC5=O)([H])[C@](C)(O)[C@H](O)C)=N%10)=O)=N8

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (75.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.6006 mL 3.0032 mL 6.0064 mL
    5 mM 0.1201 mL 0.6006 mL 1.2013 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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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: 5 mg/mL (3.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (3.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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

    Purity: 99.80%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 0.6006 mL 3.0032 mL 6.0064 mL 15.0160 mL
    5 mM 0.1201 mL 0.6006 mL 1.2013 mL 3.0032 mL
    10 mM 0.0601 mL 0.3003 mL 0.6006 mL 1.5016 mL
    15 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0011 mL
    20 mM 0.0300 mL 0.1502 mL 0.3003 mL 0.7508 mL
    25 mM 0.0240 mL 0.1201 mL 0.2403 mL 0.6006 mL
    30 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
    40 mM 0.0150 mL 0.0751 mL 0.1502 mL 0.3754 mL
    50 mM 0.0120 mL 0.0601 mL 0.1201 mL 0.3003 mL
    60 mM 0.0100 mL 0.0501 mL 0.1001 mL 0.2503 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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    Cat. No.:
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