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

MLN120B dihydrochloride  (Synonyms: ML120B dihydrochloride)

Cat. No.: HY-15473A Purity: 99.73%
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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.

For research use only. We do not sell to patients.

MLN120B dihydrochloride Chemical Structure

MLN120B dihydrochloride Chemical Structure

CAS No. : 1782573-78-7

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10 mg USD 200 In-stock
25 mg USD 420 In-stock
50 mg USD 720 In-stock
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Based on 27 publication(s) in Google Scholar

Other Forms of MLN120B dihydrochloride:

MLN120B dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    MLN120B dihydrochloride purchased from MedChemExpress. 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 MedChemExpress. 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.

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    IKK-α IKK-β IKK IKKε TBK1

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    Description

    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].

    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].

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

    MLN120B dihydrochloride Related Antibodies

    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.
    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].

    MedChemExpress (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.
    Molecular Weight

    439.72

    Formula

    C19H17Cl3N4O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    ClC1=C(C(NC(C2=CC=CN=C2C)=O)=C3C(C4=C(N3)C=NC=C4)=C1)OC.Cl.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (37.91 mM; ultrasonic and warming and adjust pH to 8 with NaOH and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo Dissolution Calculator
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    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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
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    MLN120B dihydrochloride Related Classifications

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    • 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:

    MLN120B1782573-78-7ML120BIKKIκB kinaseI kappa B kinaserheumatoid arthritismyeloma cellMM.1SMM.1RRPMI 8226RPMI-LR5RPMI-Dox40U266cancerInhibitorinhibitorinhibit

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