产品描述:
MLN120B is an inhibitor of IκB kinase β (IKKβ; IC50 = 45 nM).{58251} It is selective for IKKβ over a panel of 30 tyrosine and serine/threonine kinases (IC50s = >50 µM for all). MLN120B inhibits NF-κB activation induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) with an IC50 value of 2.8 µM in a reporter assay. It inhibits proliferation in a panel of six multiple myeloma cancer cell lines, including cell lines resistant to dexamethasone (Item No. 11015), melphalan (Item No. 16665), or doxorubicin (Item No. 15007), in a concentration-dependent manner.{58252} MLN120B (50 mg/kg) reduces serum levels of soluble human IL-6 receptor, a marker of INA-6 cell growth, in a SCID-hu mouse model of bone marrow-engrafted INA-6 multiple myeloma. It reduces paw swelling, as well as cartilage destruction and bone erosion in the inflamed joints, in a rat model of rheumatoid arthritis induced by complete Freund's adjuvant (CFA) with a median effective dose (MED) of 12 mg/kg.{58253}