Takinib

Takinib is a TGF-beta-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM). It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-alpha-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-alpha-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-alpha-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.Formal Name: N1-(1-propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide. CAS Number: 1111556-37-6. Molecular Formula: C18H18N4O2. Formula Weight: 322.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5mg/mL, DMSO: 5mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL. lambdamax: 323 nm. SMILES: O=C(C1=CC=CC(C(N)=O)=C1)NC2=NC3=CC=CC=C3N2CCC. InChi Code: InChI=1S/C18H18N4O2/c1-2-10-22-15-9-4-3-8-14(15)20-18(22)21-17(24)13-7-5-6-12(11-13)16(19)23/h3-9,11H,2,10H2,1H3,(H2,19,23)(H,20,21,24). InChi Key: UOZVVPXKJGOFIG-UHFFFAOYSA-N.