MLN120B

MLN120B is an inhibitor of IkappaB kinase beta (IKKbeta, IC50 = 45 nM). It is selective for IKKbeta over a panel of 30 tyrosine and serine/threonine kinases (IC50s = >50 µM for all). MLN120B inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (TPA, Cay-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 (Cay-11015), melphalan (Cay-16665), or doxorubicin (Cay-15007), in a concentration-dependent manner. 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.Formal Name: (9CI, ACI)-N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide. CAS Number: 783348-36-7. Molecular Formula: C19H15ClN4O2. Formula Weight: 366.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml. SMILES: O=C(C1=CC=CN=C1C)NC2=C(C(Cl)=CC3=C2NC4=C3C=CN=C4)OC. InChi Code: InChI=1S/C19H15ClN4O2/c1-10-11(4-3-6-22-10)19(25)24-17-16-13(8-14(20)18(17)26-2)12-5-7-21-9-15(12)23-16/h3-9,23H,1-2H3,(H,24,25). InChi Key: ZNOLRTPMNMPLHY-UHFFFAOYSA-N.