1. Cell Cycle/DNA Damage Autophagy
  2. CDK Autophagy
  3. Cucurbitacin E

Cucurbitacin E  (Synonyms: 葫芦素 E; α-Elaterin; α-Elaterine)

目录号: HY-N0417 纯度: 99.92%
COA 产品使用指南

Cucurbitacin E 是来自葫芦科的一种天然化合物。Cucurbitacin E 显著抑制 cyclin B1/CDC2 复合物的活性。

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Cucurbitacin E Chemical Structure

Cucurbitacin E Chemical Structure

CAS No. : 18444-66-1

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10 mM * 1 mL in DMSO ¥1470
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1 mg ¥548
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5 mg ¥1200
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10 mg ¥1900
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Customer Review

Other Forms of Cucurbitacin E:

    Cucurbitacin E purchased from MCE. Usage Cited in: Signal Transduct Target Ther. 2020 May 20;5(1):56.  [Abstract]

    Western Blot is performed to determine the protein levels of cyclin B1, Cdk1, and p-Drp1 Ser616. LMP1-positive cells are treated with or without cucurbitacin E (10 μM) for 24 h.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.

    IC50 & Target[1]

    cyclin B1/CDC2

     

    Autophagy

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HeLa IC50
    0.1 μM
    Compound: 12
    Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
    Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
    [PMID: 21459003]
    HepG2 IC50
    15.25 μM
    Compound: 12
    Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
    Cytotoxicity against human HepG2 cells after 24 hrs assessed as inhibition of cell viability by MTT assay
    [PMID: 21459003]
    HepG2 EC50
    3.2 μM
    Compound: 12
    Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
    Hepatoprotective activity in human HepG2 cells assessed as inhibition of CCl4-induced toxicity after 24 hrs by MTT assay
    [PMID: 21459003]
    HL-60 IC50
    18 nM
    Compound: 1
    Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human HL60 cells after 72 hrs by WST-8 assay
    [PMID: 20347305]
    HSC-T6 EC50
    0.04 μM
    Compound: 12
    Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
    Antiproliferative activity against serum-stimulated rat HSC-T6 cells after 24 hrs by MTT assay
    [PMID: 21459003]
    HSC-T6 IC50
    2.03 μM
    Compound: 12
    Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
    Cytotoxicity against rat HSC-T6 cell after 24 hrs by MTT assay
    [PMID: 21459003]
    HT-1080 IC50
    40 nM
    Compound: 1
    Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human HT1080 cells after 72 hrs by WST-8 assay
    [PMID: 20347305]
    JY IC50
    0.18 μM
    Compound: 1
    Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
    Inhibition of LFA1 expressed in human JY cells interaction with ICAM1-IG expressed in human HeLa cell monolayer after 45 mins by cell adhesion assay
    [PMID: 7852999]
    MCF7 IC50
    0.055 μM
    Compound: 8
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay
    [PMID: 25756299]
    U-937 IC50
    16 nM
    Compound: 1
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    Cytotoxicity against human U937 cells after 72 hrs by WST-8 assay
    [PMID: 20347305]
    体外研究
    (In Vitro)

    为了探索Cucurbitacin E (CuE) 对结直肠癌 (CRC) 细胞的抗肿瘤活性,启动了一项体外研究,其中每个 CRC 细胞系暴露于增加剂量的Cucurbitacin E (0、2.5、5 和 7.5 μM) 在 24 小时内。然后使用 MTT 方法测量Cucurbitacin E 处理的癌细胞的增殖。Cucurbitacin E 显示可诱导原发性结肠癌细胞的形态学变化。显微镜观察表明,在接触Cucurbitacin E (5 μM) 6 至 24 小时后,原发性结肠癌细胞的形态发生了显著变化。Cucurbitacin E 通过 GADD45γ 基因表达和阻断原代 CRC 细胞中的细胞周期蛋白 B1/CDC2 复合物使细胞周期停滞在 G2/M 期,从而抑制肿瘤生长[1]

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

    体内研究
    (In Vivo)

    Cucurbitacin E (0.5mg/kg) 处理的 HFD-MetS 小鼠的体重显著降低,脂肪垫重量减少[2]

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

    分子量

    556.69

    Formula

    C32H44O8

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    葫芦素 E

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 50 mg/mL (89.82 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7963 mL 8.9817 mL 17.9633 mL
    5 mM 0.3593 mL 1.7963 mL 3.5927 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.49 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.49 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.92%

    参考文献
    Cell Assay
    [1]

    The colorectal cancer (CRC) cells are seeded into 96-well culture plates at 5000 cells/well. The cells are treated with 0, 2.5, 5, and 7.5 μM Cucurbitacin E for 1-3 days. MTT dye (1 mg/mL) is added to each well for at least 4 h of treatment. The reaction is stopped by the addition of DMSO, and optical density is measured at 540 nm on a multi-well plate reader. Background absorbance of the medium in the absence of cells is subtracted. All samples are assayed in triplicate, and the mean for each experiment is calculated. Results are expressed as a percentage of control, which is considered as 100%. Each assay is carried out in triplicate, and the results are expressed as the mean[1].

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

    Animal Administration
    [2]

    Mice[2]
    C57BL/6 male mice are used. The mice are designated as metabolic syndrome mice (HFD-MetS-mice). Briefly, the mice are randomly assigned into two groups according to their diet for 8 weeks (n = 10-12): high fat diet group (HFD) (60% fat, 20% carbohydrate, 20% protein) or the matched low fat, standard diet group (SD) (10% fat, 70% carbohydrate, 20% protein). After eight weeks on high fat diet, the mice with significant obese phenotype and fasting blood glucose levels ≥126 mg/dL are considered MetS mice. The MetS mice are continued on the HFD throughout the study. The MetS mice are then randomly divided into three additional groups, according to the treatment administered by oral gavage for 10 weeks (n=10-12): a low dose 0.25 mg/kg/day of Cucurbitacin E designated as HFD+Cucurbitacin E (L) or high dose 0.5 mg/kg/day of Cucurbitacin E, designated as HFD+Cucurbitacin E (H) or 50 mg/kg/day Orlistat (HFD+Orlistat). Animals on SD are administered 0.5% CMC by oral gavage[2].

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

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7963 mL 8.9817 mL 17.9633 mL 44.9083 mL
    5 mM 0.3593 mL 1.7963 mL 3.5927 mL 8.9817 mL
    10 mM 0.1796 mL 0.8982 mL 1.7963 mL 4.4908 mL
    15 mM 0.1198 mL 0.5988 mL 1.1976 mL 2.9939 mL
    20 mM 0.0898 mL 0.4491 mL 0.8982 mL 2.2454 mL
    25 mM 0.0719 mL 0.3593 mL 0.7185 mL 1.7963 mL
    30 mM 0.0599 mL 0.2994 mL 0.5988 mL 1.4969 mL
    40 mM 0.0449 mL 0.2245 mL 0.4491 mL 1.1227 mL
    50 mM 0.0359 mL 0.1796 mL 0.3593 mL 0.8982 mL
    60 mM 0.0299 mL 0.1497 mL 0.2994 mL 0.7485 mL
    80 mM 0.0225 mL 0.1123 mL 0.2245 mL 0.5614 mL
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