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MLN120B

Catalog No. TQ0306   CAS 783348-36-7

MLN120B is a selective and ATP competitive IKKβ inhibitor (IC50: 60 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
MLN120B Chemical Structure
MLN120B, CAS 783348-36-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 45.00
2 mg In stock $ 64.00
5 mg In stock $ 97.00
10 mg In stock $ 163.00
25 mg In stock $ 347.00
50 mg In stock $ 597.00
100 mg In stock $ 817.00
1 mL * 10 mM (in DMSO) In stock $ 118.00
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Purity: 98.86%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MLN120B is a selective and ATP competitive IKKβ inhibitor (IC50: 60 nM).
Targets&IC50 IKKβ:60 nM
In vitro MLN120B almost completely blocks the 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 [2].
Cell Research 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 [1].
Animal Research Human fetal long bone grafts are implanted into SCID mice (SCID-hu mice). Approximately 4 weeks following bone implantation, 2.5×10^6 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 the detection of measurable shuIL-6R in mouse sera [1].
Molecular Weight 366.8
Formula C19H15ClN4O2
CAS No. 783348-36-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (81.78 mM)

H2O: Insoluble

TargetMolReferences and Literature

1. Hideshima T, et all. MLN120B, a novel IkappaB kinase beta inhibitor, blocks multiple myeloma cell growth in vitro and in vivo. Clin Cancer Res. 2006 Oct 1;12(19):5887-94. 2. Schopf L, et al. IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis. Arthritis Rheum. 2006 Oct;54(10):3163-73. 3. Ansaldi D, et al. Imaging pulmonary NF-kappaB activation and therapeutic effects of MLN120B and TDZD-8. PLoS One. 2011;6(9):e25093.

Related compound libraries

This product is contained In the following compound libraries:
NO PAINS Compound Library NF-κB Signaling Compound Library Orally Active Compound Library Anti-Liver Cancer Compound Library Anti-Prostate Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library

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Keywords

MLN120B 783348-36-7 NF-Κb IκB/IKK ML120B Inhibitor I kappa B kinase inhibit IKK IκB kinase MLN-120B inhibitor

 

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