tcsc1291 MLN120B

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

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].