1. Stem Cell/Wnt TGF-beta/Smad PI3K/Akt/mTOR Apoptosis
  2. TGF-beta/Smad PI3K Apoptosis
  3. Disitertide TFA

Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer.

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

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Disitertide TFA Chemical Structure

Disitertide TFA Chemical Structure

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Top Publications Citing Use of Products

    Disitertide TFA purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jan;28(1):219-232.  [Abstract]

    LINC00941-overexpressing cells treated with Disitertide (10 μM) shows increased mRNA and protein levels of ZO-1 and Ecadherin compared with controls. LINC00941-silenced cells show decreased mRNA and protein levels of ZO-1 and E-cadherin but increased mRNA and protein levels of Vimentin, Fibronectin, and Twist1.
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    Description

    Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide TFA is also a PI3K inhibitor and an apoptosis inducer[1][2][3][4][5].

    IC50 & Target

    TGF-β1, P13K[1][2].

    In Vitro

    Disitertide (P144, 100 μg/mL) TFA suppresses the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells[2].
    ? Disitertide (TGF-β1 inhibitor) TFA abrogates the MACC1- AS1 expression in GC cells, suggesting that targeting TGFβ signaling pathway may be a potential strategy to inhibit MSC-induced stemness and chemoresistance[3].
    ? Disitertide (10 μg/mL to 200 μg/mL) TFA affects proliferation, induces apoptosis as well as anoikis in A172 and U-87 MG GBM cell lines[5].

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

    Western Blot Analysis[2]

    Cell Line: Mouse embryo osteoblast precursor MC3T3-E1 cells.
    Concentration: 100 μg/mL.
    Incubation Time: 4 h.
    Result: Significantly suppressed the protein expression levels of PI3K and p-Akt, and induce the protein expression of Bax in MC3T3-E1 cells compared with the miR-590 group.
    In Vivo

    Disitertide (P144, Topical application, 300 μg/mL) TFA may promote scar maturation and improvement of hypertrophic scar morphology features in an “in vivo” model in nude mice after two weeks of treatment[4].

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

    Animal Model: Human hypertrophic scars were implanted in 60 nude mice[4].
    Dosage: 300 μg/mL was added the Lipogel.
    Administration: Topical application daily administered.
    Result: Successful shedding was achieved in 83,3% of the xenografts.
    Clinical Trial
    Molecular Weight

    1580.82 (free acid)

    Formula

    C68H109N17O22S2.xC2HF3O2

    Appearance

    Solid

    Color

    Off-white to light yellow

    Sequence

    Thr-Ser-Leu-Asp-Ala-Ser-Ile-Ile-Trp-Ala-Met-Met-Gln-Asn

    Sequence Shortening

    TSLDASIIWAMMQN

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Sealed storage, away from moisture and light

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

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

    Solvent & Solubility
    In Vitro: 

    H2O : < 0.1 mg/mL (insoluble)

    • Molarity Calculator

    • Dilution Calculator

    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

    Concentration (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: 2.5 mg/mL (Infinity mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (Infinity mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (25.0 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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
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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:
    Disitertide TFA
    Cat. No.:
    HY-P0118A
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