1. NF-κB
  2. IKK
  3. MLN120B

MLN120B  (Synonyms: ML120B)

目录号: HY-15473 纯度: 99.76%
COA 产品使用指南

MLN120B (ML120B) 是一种有效的、ATP 竞争性的和具有口服活性的 IKKβ 抑制剂,IC50 为 60 nM。MLN120B 在体内外抑制多发性骨髓瘤细胞生长,也可用于类风湿关节炎的相关研究。

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MLN120B Chemical Structure

MLN120B Chemical Structure

CAS No. : 783348-36-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1210
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1 mg ¥500
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5 mg ¥1100
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10 mg ¥1850
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25 mg ¥4200
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50 mg ¥5847
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500 mg   询价  

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Customer Review

Other Forms of MLN120B:

    MLN120B purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59.  [Abstract]

    Effects of NF-κB inhibitor (10 μM MLN120B) is measured on p62 protein in LPS-induced RAW264.7 cells.

    MLN120B purchased from MCE. Usage Cited in: J Invest Dermatol. 2017 Dec;137(12):2532-2543.  [Abstract]

    MZ B cells are pre-treated with different concentrations of MLN120B, which selectively inhibit NF-κB1 pathway, the expression of p35 and Ebi3 significantly reduced.

    查看 IKK 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

    MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis[1][2].

    IC50 & Target[4]

    IKKβ

    60 nM (IC50)

    体外研究
    (In Vitro)

    MLB120B (0-20 μM; 90 minutes) inhibits phosphorylation and degradation of IκB in RPMI 8226 and INA6 cells; however, no significant inhibition is observed in MM.1S cells[1].
    MLB120B (1.25-20 μM; 90 minutes) completely abrogates TNF-a-induced phosphorylation and degradation of IκB in a dosedependent fashion. Phosphorylation of p65 NF-κB induced by TNF-a is also blocked by MLN120B[1].
    MLN120B inhibits proliferation of multiple myeloma cell lines. MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells. Five percent to fifty percent and 18% to 70% inhibition in proliferation is observed at doses >20 uM and [3H]thymidine uptake, respectively[1].
    MLN120B (1.25-40 μM; 72 hours) almost completely blocks stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs[1].
    MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC50?values of MLN120B is 1.4 μM, 14.8 μM or 27.3 μM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3].

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

    Western Blot Analysis[1]

    Cell Line: MM.1S cells
    Concentration: 1.25-20 μM
    Incubation Time: 90 minutes
    Result: Inhibited p- IκB and p-P65 expression in a dose-dependent manner.

    Cell Viability Assay[1]

    Cell Line: Multiple myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
    Concentration: 1.25 μM-20 μM
    Incubation Time: 72 hours
    Result: Inhibits proliferation of multiple myeloma cell lines.
    体内研究
    (In Vivo)

    MLN120B (oral administration; 50 mg/kg; twice daily; 3 weeks) induces a reduction of shuIL-6R, marker of tumor growth, marker of tumor growth. It also leads to a rend toward prolonged survival in animals treated versus control[1].
    MLN120B (oral administration; 1-30 mg/kg; twice daily; 3 weeks)?inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion. NF-κB activity in arthritic joints is also reduced after MLN120B administration[2].

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

    Animal Model: Two-month-old female Lewis rats[2]
    Dosage: 30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg
    Administration: Oral administration; twice daily; 3 weeks
    Result: Protected against bone and cartilage destruction in a rat model.
    Animal Model: SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice[1]
    Dosage: 50 mg/kg
    Administration: Oral administration; twice daily; 3 weeks
    Result: Inhibited human multiple myeloma cell growth in vivo.
    分子量

    366.80

    Formula

    C19H15ClN4O2

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    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 : ≥ 31 mg/mL (84.51 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)

    * "≥" 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 2.7263 mL 13.6314 mL 27.2628 mL
    5 mM 0.5453 mL 2.7263 mL 5.4526 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.82 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 (5.67 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: 99.76%

    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 2.7263 mL 13.6314 mL 27.2628 mL 68.1570 mL
    5 mM 0.5453 mL 2.7263 mL 5.4526 mL 13.6314 mL
    10 mM 0.2726 mL 1.3631 mL 2.7263 mL 6.8157 mL
    15 mM 0.1818 mL 0.9088 mL 1.8175 mL 4.5438 mL
    20 mM 0.1363 mL 0.6816 mL 1.3631 mL 3.4079 mL
    25 mM 0.1091 mL 0.5453 mL 1.0905 mL 2.7263 mL
    30 mM 0.0909 mL 0.4544 mL 0.9088 mL 2.2719 mL
    40 mM 0.0682 mL 0.3408 mL 0.6816 mL 1.7039 mL
    50 mM 0.0545 mL 0.2726 mL 0.5453 mL 1.3631 mL
    60 mM 0.0454 mL 0.2272 mL 0.4544 mL 1.1360 mL
    80 mM 0.0341 mL 0.1704 mL 0.3408 mL 0.8520 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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    Inquiry Information

    产品名称:
    MLN120B
    目录号:
    HY-15473
    需求量: