1. NF-κB
  2. IKK
  3. MLN120B dihydrochloride

MLN120B dihydrochloride  (Synonyms: ML120B dihydrochloride)

目录号: HY-15473A 纯度: 99.73%
COA 产品使用指南

MLN120B dihydrochloride (ML120B dihydrochloride) 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 dihydrochloride Chemical Structure

MLN120B dihydrochloride Chemical Structure

CAS No. : 1782573-78-7

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Customer Review

Other Forms of MLN120B dihydrochloride:

    MLN120B dihydrochloride 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 dihydrochloride 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 dihydrochloride (ML120B dihydrochloride) 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].

    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: 5 μM; 10 μM; 20 μM
    Incubation Time: 90 mintues
    Result: Inhibited p-IκB and p-P65 expression in a dose-dependent manner.

    Cell Viability Assay[1]

    Cell Line: Myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells
    Concentration: 0-40 μM
    Incubation Time: 72 hours
    Result: Inhibited 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; 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[3].

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

    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.
    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.
    分子量

    439.72

    Formula

    C19H17Cl3N4O2

    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

    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 : 16.67 mg/mL (37.91 mM; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80°C; 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 2.2742 mL 11.3709 mL 22.7417 mL
    5 mM 0.4548 mL 2.2742 mL 4.5483 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 (sealed storage, away from moisture)。-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
    参考文献

    MLN120B dihydrochloride 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 (sealed storage, away from moisture)。-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 2.2742 mL 11.3709 mL 22.7417 mL 56.8544 mL
    5 mM 0.4548 mL 2.2742 mL 4.5483 mL 11.3709 mL
    10 mM 0.2274 mL 1.1371 mL 2.2742 mL 5.6854 mL
    15 mM 0.1516 mL 0.7581 mL 1.5161 mL 3.7903 mL
    20 mM 0.1137 mL 0.5685 mL 1.1371 mL 2.8427 mL
    25 mM 0.0910 mL 0.4548 mL 0.9097 mL 2.2742 mL
    30 mM 0.0758 mL 0.3790 mL 0.7581 mL 1.8951 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:
    MLN120B dihydrochloride
    目录号:
    HY-15473A
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