2. Stem Cell/Wnt
  3. YAP
  4. GNE-7883

GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation.

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

CAS No. : 2648450-42-2

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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 5 publication(s) in Google Scholar

GNE-7883 Related Antibodies

Top Publications Citing Use of Products

    GNE-7883 purchased from MedChemExpress. Usage Cited in: Differentiation. 2025 Jan-Feb:141:100835.  [Abstract]

    Bright-field images of E3.5 embryos treated with vehicle only (Control) or with the pan-TEAD inhibitor GNE-7883 (40 μM) from E2.5.

    GNE-7883 purchased from MedChemExpress. Usage Cited in: Differentiation. 2025 Jan-Feb:141:100835.  [Abstract]

    GNE-7883 (40 μM; E2.5 to E3.5) treatment down-regulated the TE marker genes (Cdx2, Krt18) and up-regulated the ICM marker gene (Sox2). Comparison of transcript levels between control (C) and GNE-7883 (GNE) treatment groups, as measured by quantitative RT-PCR.

    GNE-7883 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Mar 15:2025.03.13.643008.

    GNE-7883 (1 μM) effectively reduced cancer stem cells (CSCs) number.

    View All YAP Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation[1][2][3].

    IC50 & Target

    YAP/TAZ-TEAD

     

    Cellular Effect
    Cell Line Type Value Description References
    NCI-H226 IC50
    0.082 μM
    Compound: GNE-7883
    Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
    Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
    		[PMID: 35763499]
    In Vitro

    GNE-7883 exhibits strong dose-dependent antiproliferative effects in both OVCAR-8 and NCI-H226 cells, with EC50 values ​​of 115 nM and 333 nM, respectively[3].

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

    GNE-7883 Related Antibodies
    In Vivo

    GNE-7883 (100 and 250 mg/kg; s.c.; once daily for 4 days) induces tumor growth arrest in NCI-H226 xenograft mice and tumor regression in MSTO-211H xenograft mice[1].

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

    Animal Model: Mesothelioma NCIH226 xenograft mouse model[3]
    Dosage: 250 mg/kg
    Administration: Subcutaneous injection (s.c.); Once a day for 4 days
    Result: Had a strong inhibitory effect on tumor growth in vivo, with an inhibition rate of 102%.
    Molecular Weight

    500.57

    Formula

    C28H29FN6O2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C=C(C1=CC=C(C2CCCCC2)C=C1)N3)N4C3=C(C(N5CC(CF)C5)=O)C(C6=NC=CN=C6C)=N4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (99.89 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 1.9977 mL 9.9886 mL 19.9772 mL
    5 mM 0.3995 mL 1.9977 mL 3.9954 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. 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)

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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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    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: 2.5 mg/mL (4.99 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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 (4.99 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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
    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).
    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: 99.54%

    SDS (251 KB)

    COA (250 KB) HNMR (304 KB) RP-HPLC (225 KB) LCMS (97 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, 6 months; -20°C, 1 month. 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 1.9977 mL 9.9886 mL 19.9772 mL 49.9431 mL
    5 mM 0.3995 mL 1.9977 mL 3.9954 mL 9.9886 mL
    10 mM 0.1998 mL 0.9989 mL 1.9977 mL 4.9943 mL
    15 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3295 mL
    20 mM 0.0999 mL 0.4994 mL 0.9989 mL 2.4972 mL
    25 mM 0.0799 mL 0.3995 mL 0.7991 mL 1.9977 mL
    30 mM 0.0666 mL 0.3330 mL 0.6659 mL 1.6648 mL
    40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2486 mL
    50 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9989 mL
    60 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8324 mL
    80 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
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    GNE-7883 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:

    GNE-78832648450-42-2GNE7883GNE 7883YAPYes-associated proteincell proliferationcancerYAP/TAZInhibitorinhibitorinhibit

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