Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N1-(1-propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide
Purity: ≥98%
Formula Markup: C18H18N4O2
Formula Weight: 322.4
CAS Number: 1111556-37-6
Notes: Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).{40308} 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-α-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-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-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.{57119}
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