1. NF-κB Autophagy Apoptosis
  2. NF-κB Autophagy Mitophagy Apoptosis
  3. Parthenolide

Parthenolide  (Synonyms: 小白菊内酯; (-)-Parthenolide)

目录号: HY-N0141 纯度: 98.54%
COA 产品使用指南

Parthenolide是在药草短舌匹菊中发现的倍半萜内酯。 Parthenolide通过抑制 NF-κB 活化而表现出抗炎活性; 它还可抑制 HDAC1 蛋白而不影响其他I/II类HDAC。

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Parthenolide Chemical Structure

Parthenolide Chemical Structure

CAS No. : 20554-84-1

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10 mM * 1 mL in DMSO ¥550
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50 mg ¥500
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100 mg ¥700
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200 mg ¥1100
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Top Publications Citing Use of Products

    Parthenolide purchased from MCE. Usage Cited in: Cell Death Discov. 2020 Oct 6;6:97.  [Abstract]

    Representative Western blot band shows the levels of total protein (HDAC1, p65, STAT1, STAT3, and STAT6) and phosphorylated protein for the indicated molecules (p65, STAT1, STAT3, and STAT6) in BV2 cells under LPS or IL-4 stimulation for 24 h in the presence or absence of Parthenolide (PN) (1 μM).

    Parthenolide purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 1;428:77-89.  [Abstract]

    Western blots show that the NF-κB inhibitors BAY11-7082, Parthenolide, and JSH-23 cause dramatic time- and dose-dependent reductions in MGMT protein expression in LN18 and T98G glioma cells.

    查看 NF-κB 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.

    IC50 & Target[1]

    NF-κB

     

    Autophagy

     

    Mitophagy

     

    体外研究
    (In Vitro)

    Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells, indicating that apoptosis is trigged after Parthenolide exposure. In addition to induction of apoptosis, Parthenolide also induces G0/G1 cell cycle arrest in a concentration-dependent manner in A549 cells and G2/M cell cycle arrest in H1792 cells[2].

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

    体内研究
    (In Vivo)

    Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect in Phb1 KO hepatocytes. Indeed, TSA and Parthenolide-treated hepatocytes showed increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a results of specific HDAC inhibition, resulting in the attenuation of the Phb1 KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL in Phb1 KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to control Phb1 KO mice[3].

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

    Clinical Trial
    分子量

    248.32

    Formula

    C15H20O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    小白菊内酯;银胶菊内酯

    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
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (402.71 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.0271 mL 20.1353 mL 40.2706 mL
    5 mM 0.8054 mL 4.0271 mL 8.0541 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 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

    In Vivo:

    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (10.07 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。

    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (8.38 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。
    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: 98.54%

    参考文献
    Cell Assay
    [2]

    Human lung cancer cell lines are seeded in 96-well plates and treated on the second day with the given concentration of Parthenolide (0, 5, 10, 20 μM) for another 48 hours and then subjected to SRB or MTT assay. For SRB assay, live cell number is estimated as described earlier. After treatment, the medium is discarded firstly. In order to fix the adherent cells, 100 μL of cold trichloroacetic acid (10% (w/v)) are adding to each well and incubating at 4°C for at least 1 hour. The plates are then washed five times with deionized water and dried in the air. Each well are then added with 50 μL of SRB solution (0.4% w/v in 1% acetic acid) and incubated for 5 min at room temperature. The plates are washed five times with 1% acetic acid to remove unbound SRB and then air dried. The residual bound SRB is solubilized with 100 μL of 10 mM Tris base buffer (pH 10.5), and then read using a microtiter plate reader at 495 nm. The MTT assay is executed. 20 μL MTT (5 mg/mL) are added to each sample and incubate at 37°C for 4 h, then 100 μL solubilization solution are added. Cell viability is determined at 595 nm[2].

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

    Animal Administration
    [3]

    Mice[3]
    Phb1 KO mice are used. Males from 8-12 weeks of age are treated. Parthenolide is intraperitoneally injected at a dose of 3 mg/kg 24 h and 1h before bile duct ligation (BDL) or twice a week during two weeks. Liver specimens are snap-frozen for subsequent analysis[3].

    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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.0271 mL 20.1353 mL 40.2706 mL 100.6765 mL
    5 mM 0.8054 mL 4.0271 mL 8.0541 mL 20.1353 mL
    10 mM 0.4027 mL 2.0135 mL 4.0271 mL 10.0677 mL
    15 mM 0.2685 mL 1.3424 mL 2.6847 mL 6.7118 mL
    20 mM 0.2014 mL 1.0068 mL 2.0135 mL 5.0338 mL
    25 mM 0.1611 mL 0.8054 mL 1.6108 mL 4.0271 mL
    30 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3559 mL
    40 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5169 mL
    50 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0135 mL
    60 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6779 mL
    80 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
    100 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
    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:
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    目录号:
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