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

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

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Disitertide diammonium) that retains the same biological activity.

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

Custom Peptide Synthesis

Disitertide Chemical Structure

Disitertide Chemical Structure

CAS No. : 272105-42-7

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Top Publications Citing Use of Products

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

    In Vitro

    Disitertide (P144, 100 μg/mL) 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) 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) 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 (Topical application, 300 μg/mL) 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

    Formula

    C68H109N17O22S2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    Sequence Shortening

    TSLDASIIWAMMQN

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Sealed storage, away from moisture and light, under nitrogen

    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, under nitrogen)

    Solvent & Solubility
    In Vitro: 

    H2O

    Peptide Solubility and Storage Guidelines:

    1.  Calculate the length of the peptide.

    2.  Calculate the overall charge of the entire peptide according to the following table:

      Contents Assign value
    Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
    Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
    Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

    3.  Recommended solution:

    Overall charge of peptide Details
    Negative (<0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, add NH4OH (<50 μL).
    3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
    Positive (>0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
    3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
    Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
    2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (1.58 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (1.58 mM); Clear solution

    Purity & Documentation
    References
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    • Molarity Calculator

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    The molarity calculator equation

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

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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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
    Cat. No.:
    HY-P0118
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