MLN120B

SKU: orb1296064

Description

MLN120B is a potent, ATP-competitive small molecule inhibitor of IKKβ with an IC50 of 60 nM. It is a valuable research tool for studying NF-κB signaling in inflammatory and oncological contexts, applicable in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 783348-36-7
• MW: 366.8
• Purity: 98.92%
• Formula: C₁₉H₁₅ClN₄O₂
• SMILES: COc1c(Cl)cc2c3ccncc3[nH]c2c1NC(=O)c1cccnc1C
• Target: IκB/IKK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.45 mM);DMSO:30 mg/mL (81.79 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  IKKβ:60 nM
• In Vivo:
  MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth in vivo . 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 .
• 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 . 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 .
• 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 .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IKK, IkB, IkB/IKK, Inhibitor, I kappa B kinase, inhibit, IκB, IκB kinase, IKKβ, MLN120B, MLN-120B, ML120B

Compound Identifiers

PubChem CID

9929127