1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. GW4869

GW4869 是非竞争性的中性鞘磷脂酶 (N-SMase)抑制剂,IC50值为1 μM。GW4869 是外泌体合成/释放的抑制剂。

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GW4869 Chemical Structure

GW4869 Chemical Structure

CAS No. : 6823-69-4

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Customer Review

MCE 顾客使用本产品发表的 133 篇科研文献

RT-PCR
WB
IF
Proliferation Assay

    GW4869 purchased from MCE. Usage Cited in: Protein Cell. 21 September 2022.

    The TAZ protein level in PCDH and NDFIP1-OE SPC-A1 and A549 cells with or without GW4869 (5 μM; 24 h).

    GW4869 purchased from MCE. Usage Cited in: Nat Commun. 2022 Aug 1;13(1):4461.  [Abstract]

    Immunoblot analysis of TβRII in whole cells lysate and EVs from MDA-MB-231 cells with GW4869 (10 μM) treatment for 48 h. Pre-treatment of cells with GW4869, which inhibits the release of extracellular vesicles, also sharply reduced the TβRII levels in the TEVs

    GW4869 purchased from MCE. Usage Cited in: Theranostics. 2022 Sep 6;12(15):6527-6547.  [Abstract]

    The hEECs are pre-treated with 0.1% DMSO or 1 µM GW4869 for 24 h, and then co-cultured with isolated endometrial NK cells for another 24 h, in vitro.

    GW4869 purchased from MCE. Usage Cited in: Cell Death Dis. 2022 Mar 26;13(3):271.  [Abstract]

    WB analysis of CD63 and CD81 in exosomes extracted from MSC-conditioned medium and GW4869 (10 µM) pretreated MSC-conditioned medium.

    GW4869 purchased from MCE. Usage Cited in: Cell Death Dis. 2022 Apr 20;13(4):382.  [Abstract]

    Western blotting is used to detect TIMP2 expression in Caki-1 cells and 786-O cells after adding GW4869 (5 μM) to the coculture system.

    GW4869 purchased from MCE. Usage Cited in: Adv Mater. 2021 Dec;33(49):e2103471.  [Abstract]

    Whole cells lysate and EVs derived from Vero-E6 cells treated with control DMSO or GW4869 (10 μM) for 48 h. Pre‐treatment of cells with GW4869, which inhibits the release of extracellular vesicles, also reduced the ACE2 levels in EVs.

    GW4869 purchased from MCE. Usage Cited in: J Extracell Vesicles. 2021 Feb;10(4):e12068.  [Abstract]

    Representative actin ring and TRAP staining images of BMMs cultured with PC3‐CM depleted EVs using ultracentrifugation or GW4869 (10 μM; 6 h).

    GW4869 purchased from MCE. Usage Cited in: Biomaterials. 2021 Dec;279:121223.

    The results also show higher expression of tooth development-related proteins (GLI2, GLI3, DLX1, BMP-2, BMP-4), dentinogenesis-related proteins (DSPP, DMP-4) and cementogenesis-related proteins (CAP, CEMP) in the DA-Exo and GW4869+DA-Exo groups than in the GW4869 (20 μM; 24 h) and hDPSC groups.

    GW4869 purchased from MCE. Usage Cited in: Engineering. 19 October 2021.

    In SNU-449 cells, GW4869 (20 μM; 24 h) into the co-culture system and observed that the Cy3-fluorescence of the recipient cells is dramatically weakened.

    GW4869 purchased from MCE. Usage Cited in: Mol Ther-Nucl Acids. 2021 Apr 24;24:923-938.  [Abstract]

    The diameter of myotubes and the MHC protein expression of the GW4869-treated C26 group were higher than the control C26 group.

    GW4869 purchased from MCE. Usage Cited in: Mol Ther-Nucl Acids. 2021 Apr 24;24:923-938.  [Abstract]

    The pro-atrophy ability of C26 tumor medium is inhibited by GW4869.

    GW4869 purchased from MCE. Usage Cited in: Cell Rep. 2021 Jan 5;34(1):108576.  [Abstract]

    M1 macrophages are treated with bmiR-29-Exos with or without 10 μM GW4869 for 48 h; then, relative miR-29a expression in macrophages is determined by qPCR.

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

    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.  [Abstract]

    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.  [Abstract]

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

    查看 Phospholipase 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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]

    体外研究
    (In Vitro)

    GW4869 (10 μM) 部分抑制 TNF 诱导的鞘磷脂 (SM) 水解,20 μM 的化合物可完全防止 SM 损失。添加 10 -20 μM GW4869 可完全抑制神经酰胺的初始积累,而这种作用在稍后的时间点 (24 小时) 会部分消失。GW4869 的作用发生在谷胱甘肽下降的下游。GW4869 能够以剂量依赖性方式显著防止细胞死亡[1]
    GW4869 (10 或 20 μM) 抑制外泌体释放和促炎细胞因子的产生巨噬细胞。GW4869 抑制神经酰胺介导的多泡体 (MVB) 向内出芽和从 MVB 释放成熟外泌体[2]
    GW4869 还可以逆转 CCN2 3'-UTR 活性的抑制肝星状细胞中富含 miR-214 的外泌体[3]
    溶解注意事项:GW4869 通常用 DMSO 配置悬浮液作为储备液,分装储存在 -80℃。

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

    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.
    体内研究
    (In Vivo)

    GW4869 (2.5 μg/g,腹腔注射) 抑制小鼠的外泌体释放,从而阻断 LPS 刺激的促炎细胞因子产生和心脏炎症。GW4869 减轻 LPS 引起的心肌功能障碍并提高小鼠的存活率[2]
    GW4869 (2.5 μg/g,ip) 阻断 CLP 小鼠促炎细胞因子的产生和心脏炎症[2]

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

    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 (2.5 μg/g, 100 μL)).
    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.
    分子量

    577.50

    Formula

    C30H30Cl2N6O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 0.1 mg/mL (0.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    *GW4869 is usually formulated as a suspension.

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 98.86%

    参考文献
    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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    产品名称:
    GW4869
    目录号:
    HY-19363
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