2. NF-κB
  3. NF-κB
  4. (-)-DHMEQ

(-)-DHMEQ  (Synonyms: Dehydroxymethylepoxyquinomicin)

目录号: HY-14645 纯度: 99.37%
COA 产品使用指南

摩尔计算器

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) 是一种有效，选择性且不可逆的 NF-κB 抑制剂，与半胱氨酸残基共价结合。(-)-DHMEQ 抑制 NF-κB 的核易位，并显示抗炎和抗癌活性。

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(-)-DHMEQ Chemical Structure

(-)-DHMEQ Chemical Structure

CAS No. : 287194-40-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1650
In-stock
2 mg ￥1150
In-stock
5 mg ￥1980
In-stock
10 mg ￥3000
In-stock
25 mg ￥5300
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of (-)-DHMEQ:

(-)-DHMEQ 相关抗体

Top Publications Citing Use of Products

    (-)-DHMEQ purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Jun;17(6):1303-1314.  [Abstract]

    Effects of TNF-α/DHMEQ on the expression of NF-κB and AR as well as neoplastic transformation of urothelial cells. Western blotting of NF-κB/p65, p-NF-κB/p65, and AR, using proteins extracted from SVHUC-AR cells cultured with ethanol, TNF-α(20 ng/mL), or DHMEQ (15 µg/mL) for 6 hours.

    (-)-DHMEQ purchased from MCE. Usage Cited in: Mol Cancer Ther. 2018 Jun;17(6):1303-1314.  [Abstract]

    Effects of NF-κB activation/inhibition on the expression of NF-κB and its downstream targets as well as AR in bladder cancer cells. Western blotting of NF-κB/p65, p-NF-κB/p65, and AR, using proteins extracted from UMUC3 cells cultured with ethanol (mock), TNF-α (20 ng/mL), or DHMEQ (15 µg/mL) for 6 hours.

    (-)-DHMEQ purchased from MCE. Usage Cited in: Mol Cells. 2018 Dec 31;41(12):1008-1015.  [Abstract]

    NCI-H157 cells are pretreated with DHMEQ (10 or 20 μg/mL) for 2 h and then stimulated with PS-341 for 6 or 24 h. Nuclear proteins (6 h) and whole cell proteins (24 h) are isolated and subjected to Western blot analysis for p65, Lamin A/C, COX-2, and GAPDH.

    (-)-DHMEQ purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1669-1677.  [Abstract]

    A549 transfectants stably expressing RelB (C144S) (B) are preincubated with various concentrations of (–)-DHMEQ for 1 h and then incubated with or without LTβ (25 ng/mL) for 2 h in the presence or absence of (−)-DHMEQ.

    (-)-DHMEQ purchased from MCE. Usage Cited in: Biol Pharm Bull. 2017;40(10):1669-1677.  [Abstract]

    A549 transfectants stably expressing RelB WT (A) are preincubated with various concentrations of (–)-DHMEQ for 1 h and then incubated with or without LTβ (25 ng/mL) for 2 h in the presence or absence of (−)-DHMEQ.

    查看 NF-κB 亚型特异性产品:

    查看所有亚型
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity[1][2][3].

    IC50 & Target[1]

    RelA

     

    RelB

     

    体外研究
    (In Vitro)

    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity[2].
    ? (-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines[2].
    ? (-)-DHMEQ (10 μg/mL; 4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9[2].
    ? (-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ[2].
    ? (-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB[1].

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

    (-)-DHMEQ 相关抗体:

    Cell Proliferation Assay[2]

    Cell Line: TL-Om1, MT-1, KK-1, ST-1 and K562 cells
    Concentration: 2 μg/mL, 5 μg/mL, 10 μg/mL
    Incubation Time: 12 hours, 24 hours, 48 hours
    Result: Significantly reduced the viability of all cell lines in a dose- and time-dependent manner.

    Apoptosis Analysis[2]

    Cell Line: TL-Om1, MT-1 and K562 cells
    Concentration: 10 μg/mL
    Incubation Time: 0 hours, 24 hours, 48 hours
    Result: Annexin V-positive cells were significantly increased after 24 to 48 hours.

    Western Blot Analysis[2]

    Cell Line: MT-1 cells
    Concentration: 10 μg/mL
    Incubation Time: 4 hours, 8 hours, 16 hours
    Result: Annexin V-positive cells were significantly increased after 24 to 48 hours.
    体内研究
    (In Vivo)

    (-)-DHMEQ (4 mg/kg or 12 mg/kg; intraperitoneal injection; on day 0 and 3 times a week; for one month; SCID mice) treatment shows a significant increase in the survival rate in mice[2].

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

    Animal Model: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells[2]
    Dosage: 4 mg/kg or 12 mg/kg
    Administration: Intraperitoneal injection; on day 0 and 3 times a week; for one month
    Result: Showed a significant increase in the survival rate in mice.
    分子量

    261.23

    Formula

    C13H11NO5
    CAS 号
    性状

    固体

    颜色

    Off-white to gray

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 95 mg/mL (363.66 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 3.8280 mL 19.1402 mL 38.2804 mL
    5 mM 0.7656 mL 3.8280 mL 7.6561 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 (stored under nitrogen)。-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

    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: 5 mg/mL (19.14 mM); 悬浊液; 超声助溶

      此方案可获得 5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 50.0 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。
    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

    只
    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）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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: 99.37%

    COA (289 KB) HNMR (257 KB) RP-HPLC (244 KB)

    产品使用指南 (1538 KB)
    参考文献

    (-)-DHMEQ 相关分类

    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 (stored under nitrogen)。-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 3.8280 mL 19.1402 mL 38.2804 mL 95.7011 mL
    5 mM 0.7656 mL 3.8280 mL 7.6561 mL 19.1402 mL
    10 mM 0.3828 mL 1.9140 mL 3.8280 mL 9.5701 mL
    15 mM 0.2552 mL 1.2760 mL 2.5520 mL 6.3801 mL
    20 mM 0.1914 mL 0.9570 mL 1.9140 mL 4.7851 mL
    25 mM 0.1531 mL 0.7656 mL 1.5312 mL 3.8280 mL
    30 mM 0.1276 mL 0.6380 mL 1.2760 mL 3.1900 mL
    40 mM 0.0957 mL 0.4785 mL 0.9570 mL 2.3925 mL
    50 mM 0.0766 mL 0.3828 mL 0.7656 mL 1.9140 mL
    60 mM 0.0638 mL 0.3190 mL 0.6380 mL 1.5950 mL
    80 mM 0.0479 mL 0.2393 mL 0.4785 mL 1.1963 mL
    100 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9570 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.

    Keywords:

    (-)-DHMEQ287194-40-5DehydroxymethylepoxyquinomicinNF-κBNuclear factor-κBNuclear factor-kappaBCysteinecovalentlyp65cRelRelBp50anti-inflammatoryanticancerInhibitorinhibitorinhibit

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