2. NF-κB
  3. IKK
  4. MLN120B

MLN120B  (Synonyms: ML120B)

Cat. No.: HY-15473 Purity: 99.94%
COA Handling Instructions

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.

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

MLN120B Chemical Structure

MLN120B Chemical Structure

CAS No. : 783348-36-7

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10 mM * 1 mL in DMSO USD 145 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of MLN120B:

Top Publications Citing Use of Products

    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.

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    IKK-α IKK-β IKK IKKε TBK1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

    IKKβ

    60 nM (IC50)

    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.
    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.
    Molecular Weight

    366.80

    Appearance

    Solid

    Formula

    C19H15ClN4O2
    CAS No.
    SMILES

    O=C(C1=CC=CN=C1C)NC2=C(OC)C(Cl)=CC3=C2NC4=C3C=CN=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (84.51 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2726 mL 1.3631 mL 2.7263 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (5.67 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (5.67 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.94%

    COA (262 KB) HNMR (276 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
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    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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    Keywords:

    MLN120B783348-36-7ML120BIKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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