1. NF-κB
  2. IKK
  3. MLN120B

MLN120B (Synonyms: ML120B)

Cat. No.: HY-15473 Purity: 99.56%
Handling Instructions

MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 864 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

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

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

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    Description

    MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM.

    IC50 & Target

    IKKβ

    60 nM (IC50)

    In Vitro

    MLN120B inhibits both baseline and tumor necrosis factor-α-induced nuclear factor-κB activation, associated with down-regulation of IκBα and p65 nuclear factor-κB phosphorylation in multiple myeloma cells. MLN120B 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, 14.8 or 27.3 µM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively[3].

    In Vivo

    MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth in vivo[1]. MLN120B (12 mg/kg twice daily, p.o.) 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 reduced after MLN120B administration[2].

    Molecular Weight

    366.80

    Formula

    C₁₉H₁₅ClN₄O₂

    CAS No.

    783348-36-7

    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)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (6.82 mM); Suspended solution; Need ultrasonic

    • 2.

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

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

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Multiple myeloma cells are cultured with MLN120B, harvested, washed, and lysed using lysis buffer [50 mM Tris-HCl (pH 7.4), 150 mM NaCl, 1% NP40, 5 mM EDTA, 5 mM NaF, 2 mM Na3VO4, 1 mM phenylmethylsulfonyl fluoride, 5 μg/mL leupeptin, 5 μg/mL aprotinin]. Whole-cell lysates are subjected to Western blotting using phosphorylated IκBα, IκBα, phosphorylated p65 NF-κB, and p65 NF-κB antibodies.

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

    Animal Administration
    [1]

    Human fetal long bone grafts are implanted into SCID mice (SCID-hu mice) as described previously. Approximately 4 weeks following bone implantation, 2.5×106 INA6 multiple myeloma cells in 50 μL PBS is injected directly into human bone within SCID-hu hosts. Soluble human IL-6 receptor (shuIL-6R) released from INA6 cells is assessed in mouse sera by ELISA as in our prior studies. Mice are treated orally with vehicle alone or MLN120B 50 mg/kg (twice daily) for 3 weeks after detection of measurable shuIL-6R in mouse sera.

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

    References

    Purity: 99.56%

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    Keywords:

    MLN120BML120BIKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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