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  3. GW4869

GW4869 

Cat. No.: HY-19363 Purity: 95.26%
Handling Instructions

GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC50 of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.

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

GW4869 Chemical Structure

GW4869 Chemical Structure

CAS No. : 6823-69-4

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Customer Review

Based on 18 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GW4869 purchased from MCE. Usage Cited in: Stem Cell Res Ther. 2020 Jan 23;11(1):37.

    Exos-IL6 are added to macrophages to detect inflammatory cytokines, chemokines, and growth factors in cell culture media. GM-CSF, granulocyte-macrophage colony-stimulating factor; IL, interleukin; MIP-1, macrophage inflammatory protein-1; IP-10, interferon-inducible protein-10; MDC, macrophage-derived chemokine; MCP-1, monocyte chemoattractant protein-1; TNF-ɑ, tumor necrosis factor.

    GW4869 purchased from MCE. Usage Cited in: Int J Oncol. 2019 May;54(5):1567-1578.

    LSCC cell AMC-HN-8 is treated with 20 μM GW4869 compared with 0.5% DMSO. 20 μM GW4869 can significantly alter the levels of miR-1246 within the LSCC cells and sEV.

    GW4869 purchased from MCE. Usage Cited in: Int J Oncol. 2019 May;54(5):1567-1578.

    Western blot analysis is used to assess levels of exosome markers in hucMMSCs-exos and GW4869-treated hUCMSCs-CM.

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    Description

    GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC50 of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release[1][2][3][4].

    IC50 & Target

    IC50: 1 μM (neutral sphingomyelinase)[1]

    In Vitro

    GW4869 (10 μM) partially inhibits TNF-induced sphingomyelin (SM) hydrolysis, and 20 μM of the compound is protected completely from the loss of SM. The addition of 10-20 μM GW4869 completely inhibits the initial accumulation of ceramide, whereas this effect is partially lost at later time points (24 h). The action of GW4869 occurs downstream of the drop in glutathione. GW4869 is able, in a dose-dependent manner, to significantly protect from cell death[1].
    GW4869 (10 or 20 μM) inhibits both exosome release and pro-inflammatory cytokine production in macrophages. GW4869 inhibits the ceramide-mediated inward budding of multivesicular bodies (MVBs) and release of mature exosomes from MVBs[2].
    GW4869 also could reverse the inhibition of CCN2 3’-UTR activity by miR-214-enriched exosomes in hepatic stellate cells[3].
    Solution Attention: GW4869 is routinely stored at −80 °C as a stock suspension in DMSO.

    Cell Viability Assay[1]

    Cell Line: MCF7 human breast cancer cells.
    Concentration: 10-20 μM.
    Incubation Time: 30 min (then treated with TNF (3 nM) followed).
    Result: Significantly inhibited TNF-induced SM hydrolysis, whereas 20 μM of the compound protected completely from the loss of SM.

    Cell Viability Assay[2]

    Cell Line: Fresh RAW264.7 macrophages.
    Concentration: 10 or 20 μM.
    Incubation Time: 2 hours (then treated with 1 μg/mL LPS incubation).
    Result: LPS-triggered exosome generation was remarkably attenuated in macrophages upon pre-treatment of macrophages with 10 μM GW4869, as evidenced by a 22% reduction in the activity of AChE. Such attenuation was further enhanced by treatment with the dose of 20 μM.
    In Vivo

    GW4869 (2.5 μg/g, i.p.) causes inhibition of exosome release blocks LPS-stimulated pro-inflammatory cytokine production and cardiac inflammation in mice. GW4869 mitigates LPS-caused myocardial dysfunction and improves survival in mice[2].
    GW4869 (2.5 μg/g, i.p.) blocks the production of pro-inflammatory cytokines and cardiac inflammation in CLP mice[2].

    Animal Model: 10-12 weeks old Male wild-type C57BL/6 mice (Endotoxin-Challenged Mice)[2].
    Dosage: 2.5 μg/g.
    Administration: I.P. once (1 h later, followed by an i.p. injection of LPS (25 μg/g, 100μL)).
    Result: Significantly decreased exosome levels by 37% in sera, compared to levels collected from control mice. At 12 h after LPS injection, the levels of circulating exosomes were increased significantly compared to PBS-controls, as evidenced by a 1.7-fold elevation in the AChE activity.
    Animal Model: 10-12 weeks old Male wild-type C57BL/6 mice (CLP Polymicrobial Sepsis Model)[2].
    Dosage: 2.5 μg/g.
    Administration: I.P. once (before sham or CLP surgery).
    Result: Decreased exosome concentration by 33% compared to mice injected with PBS in sham-surgery controls.
    CLP-stimulated exosome release was significantly inhibited by pre-treatment of CLP mice compared to CLP mice pre-treated with PBS.
    Molecular Weight

    577.50

    Formula

    C₃₀H₃₀Cl₂N₆O₂

    CAS No.

    6823-69-4

    SMILES

    O=C(NC1=CC=C(C2=NCCN2)C=C1)/C=C/C3=CC=C(/C=C/C(NC4=CC=C(C5=NCCN5)C=C4)=O)C=C3.[H]Cl.[H]Cl

    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 : < 1 mg/mL (insoluble or slightly soluble)

    H2O : < 0.1 mg/mL (insoluble)

    *GW4869 is usually formulated as a suspension.

    References
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    Keywords:

    GW4869GW 4869GW-4869PhospholipaseInhibitorinhibitorinhibit

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