2. Stem Cell/Wnt
  3. YAP
  4. TED-347

TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.

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

CAS No. : 2378626-29-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 11 publication(s) in Google Scholar

TED-347 Related Antibodies

Top Publications Citing Use of Products

    TED-347 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 16;15(1):9950.  [Abstract]

    Transwell migration, invasion, foci formation assays of YAP1 downstream genes following knockdown via shRNAs targeting YAP1 or treatment with two pharmacological YAP-TEAD inhibitors (CA3 and TED-347) in GPRC5A-overexpressing KYSE30 cells.

    TED-347 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Nov 16;15(1):9950.  [Abstract]

    Immunoblotting of YAP1 downstream genes following knockdown via shRNAs targeting YAP1 or treatment with two pharmacological YAP-TEAD inhibitors (CA3 and TED-347) in GPRC5A-overexpressing KYSE30 cells.

    TED-347 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Mar 1;40(1):88.  [Abstract]

    RT-PCR analysis was used to detect the mRNA expression levels of CTGF and CYR61 in pancreatic cancer cells infected with sh-Control or sh-WDR3 #1 and treated with or without TED-347 (10 μM).

    TED-347 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Mar 1;40(1):88.  [Abstract]

    PANC-1 cells infected with sh-Control or sh-WDR3 #1 were subcutaneously injected into nude mice. The mice were treated with TED-347 3 times on days 1, 4, and 7 at a dose of 20 mg/kg. The tumor volume was decreased.

    TED-347 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Mar 1;40(1):88.  [Abstract]

    PANC-1 cells infected with sh-Control or sh-WDR3 #1 and treated with or without TED-347 (10 μM) were harvested for MTS.

    View All YAP Isoform Specific Products:

    View All Isoforms
    YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity[1].

    IC50 & Target

    YAP/TAZ-TEAD

     

    In Vitro

    TED-347 (0.5-100 μM; 48 hours) inhibits GBM43 cancer cell viability[1].
    TED-347 (5 μM; 48 hours) inhibits co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1[1].
    TED-347 (10 μM; 48 hours) shows a significant reduction in CTGF transcript levels[1].
    TED-347 (0.5-100 μM; 24 hours) reduces reporter activity in cells transfected with a TEAD reporter. TED-347 (0.5-100 μM) also inhibits TEAD4 transcriptional activity in GBM43 cells[1].
    TED-347 is selective for TEADs and inhibits TEAD2 with the same efficacy. TED-347 (0.1-100 μM; 24-48 hours) inhibits TEAD4 binding to full-length Yap1 in dose- and time-dependent manner. TED-347 (1-100 μM) shows no inhibition of uPAR uPA or Cav2.2 α β protein-protein interactions. Non-covalent binding of TED-347 to TEAD4 exhibits little change to the TEAD4 Yap1 binding affinity[1].
    TED-347 has the maximum rate of inactivation of 0.038 hours, corresponding to a t1/2∞ of 18.2 hours[1].

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

    TED-347 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: GBM43 glioblastoma cell lines
    Concentration: 0.5, 1, 10, 100 μM
    Incubation Time: 48 hours
    Result: Inhibited GBM43 cancer cell viability and inhibited GBM43 cell viability by 30% at 10 μM.

    Western Blot Analysis[1]

    Cell Line: HEK-293 cells
    Concentration: 5 μM
    Incubation Time: 48 hours
    Result: Showed a significant loss of co-immunoprecipitation of Myc-tagged TEAD4 with FLAG-tagged Yap1.

    RT-PCR[1]

    Cell Line: HEK-293 cells
    Concentration: 10 μM
    Incubation Time: 48 hours
    Result: Showed a significant reduction in CTGF transcript levels versus control cells and had no inhibition on TEAD mutant transcriptional activity and protein-protein interactions in cell culture.
    Molecular Weight

    313.70

    Formula

    C15H11ClF3NO
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2)CCl
    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 (318.78 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 3.1878 mL 15.9388 mL 31.8776 mL
    5 mM 0.6376 mL 3.1878 mL 6.3755 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.

    • 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    90% Corn Oil

      Solubility: ≥ 6.25 mg/mL (19.92 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

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

      Solubility: 2.5 mg/mL (7.97 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.
    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

    Purity: 99.13%

    SDS (554 KB)

    COA (249 KB) RP-HPLC (256 KB)

    Handling Instructions (2659 KB)
    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 3.1878 mL 15.9388 mL 31.8776 mL 79.6940 mL
    5 mM 0.6376 mL 3.1878 mL 6.3755 mL 15.9388 mL
    10 mM 0.3188 mL 1.5939 mL 3.1878 mL 7.9694 mL
    15 mM 0.2125 mL 1.0626 mL 2.1252 mL 5.3129 mL
    20 mM 0.1594 mL 0.7969 mL 1.5939 mL 3.9847 mL
    25 mM 0.1275 mL 0.6376 mL 1.2751 mL 3.1878 mL
    30 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6565 mL
    40 mM 0.0797 mL 0.3985 mL 0.7969 mL 1.9923 mL
    50 mM 0.0638 mL 0.3188 mL 0.6376 mL 1.5939 mL
    60 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3282 mL
    80 mM 0.0398 mL 0.1992 mL 0.3985 mL 0.9962 mL
    100 mM 0.0319 mL 0.1594 mL 0.3188 mL 0.7969 mL
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    TED-347 Related Classifications

    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.

    Keywords:

    TED-3472378626-29-8TED347TED 347YAPYes-associated proteinirreversiblecovalentallostericYAP-TEADprotein-proteininteractionTEAD4 Yap1Cys-367TEAD4TEADtranscriptionalantitumorYap1glioblastomaPPIInhibitorinhibitorinhibit

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