2. Metabolic Enzyme/Protease
  3. MMP
  4. GW280264X

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells.

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

CAS No. : 866924-39-2

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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 7 publication(s) in Google Scholar

GW280264X Related Antibodies

Top Publications Citing Use of Products

    GW280264X purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Apr 28:102117.  [Abstract]

    Surface staining of TNF on Pan T or NK cells from 6 donors in the presence of DMSO or GW280264X (10 μM) post-4 h PMA/ionomycin stimulation.

    GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 17;25(8):4404.

    PMA-differentiated THP-1s (for 72 h) were treated for 4 h with either 3 µM of GW280264X (GW; ADAM17 inhibitor), 5 µM of DAPT (γ-secretase inhibitor), or 10 µM of MG132 (proteasomal inhibitor).

    GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 23;25(3):1363.

    ELISA of IL6R in the supernatant of A549 after 17 h incubation with either DMSO or GW280264X (1 μM).

    GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 17;25(8):4404.

    THP-1s expressing the tagged construct were starved for 18 h in serum-free RPMI and treated for 3 h. Flow cytometry data shows positive GFPs without staining. As expected, CHX treatment after 3 h reduces the expression of the construct. Gas6-VK, used at a concentration > 10 nM, decreases the FLAG-PE signal more when compared to other treatments known to induce cleavage (PMA, LPS). GW280264X is used as a control for Mertk cleavage.

    GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 23;25(3):1363.

    Western blots of STAT3 activation status (p-STAT3/STAT3) in A549 and HEP in the following conditions: without stimulus (BL), IL6 + PBS, or IL6 + sgp130Fc in the presence of either DMSO or GW280264X (1 μM).

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    MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].

    IC50 & Target[1]

    ADAM17

    8 nM (IC50)

    ADAM10

    11.5 nM (IC50)

    In Vitro

    The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2].

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

    GW280264X Related Antibodies

    Cell Viability Assay[2]

    Cell Line: Glioblastoma-initiating cells (GIC) GS-7 cells
    Concentration: 0.1, 1, and 3 µM
    Incubation Time: 48 hours
    Result: Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.
    In Vivo

    Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI)[3].

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

    Animal Model: C57BL/6 mice[3]
    Dosage: 100  µg/kg
    Administration: I.p. injected; every day for one week starting 4 h post-surgery
    Result: Showed significantly improved functional recovery compared to the control group.
    Molecular Weight

    575.72

    Formula

    C28H41N5O6S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OCC1=CC=CC=C1)NCCCC[C@H](NC([C@H](CC(C)C)[C@@H](N(C=O)O)CCC)=O)C(NC2=NC=CS2)=O
    Shipping

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

    DMSO : 100 mg/mL (173.70 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 1.7370 mL 8.6848 mL 17.3696 mL
    5 mM 0.3474 mL 1.7370 mL 3.4739 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)

    C1

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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: ≥ 2.08 mg/mL (3.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.30%

    SDS (604 KB)

    COA (248 KB) HNMR (474 KB) RP-HPLC (252 KB) LCMS (95 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 1.7370 mL 8.6848 mL 17.3696 mL 43.4239 mL
    5 mM 0.3474 mL 1.7370 mL 3.4739 mL 8.6848 mL
    10 mM 0.1737 mL 0.8685 mL 1.7370 mL 4.3424 mL
    15 mM 0.1158 mL 0.5790 mL 1.1580 mL 2.8949 mL
    20 mM 0.0868 mL 0.4342 mL 0.8685 mL 2.1712 mL
    25 mM 0.0695 mL 0.3474 mL 0.6948 mL 1.7370 mL
    30 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4475 mL
    40 mM 0.0434 mL 0.2171 mL 0.4342 mL 1.0856 mL
    50 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8685 mL
    60 mM 0.0289 mL 0.1447 mL 0.2895 mL 0.7237 mL
    80 mM 0.0217 mL 0.1086 mL 0.2171 mL 0.5428 mL
    100 mM 0.0174 mL 0.0868 mL 0.1737 mL 0.4342 mL
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    GW280264X 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:

    GW280264X866924-39-2MMPMatrix metalloproteinasesMixedADAM10TACEADAM17metalloproteinasesimmunogenicityglioblastomaimmunotherapystemNKGICInhibitorinhibitorinhibit

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