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MLN120B

Cat. No. M8970
MLN120B Structure
Synonym:

ML120B

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MLN120B is a potent and effective, ATP competitive IKKβ inhibitor with IC50 value of 20 μM. 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.

In vivo, MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth. 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.

Protocol
Cell Experiment
Cell lines Multiple myeloma cells
Preparation method MLN-120B is dissolved in DMSO. Multiple myeloma cells are cultured with MLN-120B, 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.
Concentrations
Incubation time
Animal Experiment
Animal models Rat adjuvant-induced arthritis model (Two-month-old female Lewis rats)
Formulation
Dosages 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration orally as a suspension delivered via a gavage needle
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 366.8
Formula C19H15ClN4O2
CAS Number 783348-36-7
Purity >99%
Solubility DMSO: ≥ 20 mg/mL
Storage at -20°C
References

Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8.
Ansaldi D, et al. PLoS One. 2011;2011. PMID: 21966423.

MLN120B, a novel IkappaB kinase beta inhibitor, blocks multiple myeloma cell growth in vitro and in vivo.
Hideshima T, et al. Clin Cancer Res. 2006 Oct 1;12(19):5887-94. PMID: 17020997.

IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis.
Schopf L, et al. Arthritis Rheum. 2006 Oct;54(10):3163-73. PMID: 17009244.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MLN120B, ML120B supplier, IκB/IKK, inhibitors

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