Takinib

Takinib

CAT N°: 24161
Price:

From 48.00 40.80

Takinib is a TGF-?-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-?-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-?-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-?-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}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N1-(1-propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide
  • Correlated keywords
    • RA interleukin IL6 p 38 MAPK 8 9 cJun TNF? TGF? TAK IRAK IRAK 4 Clk 2 MINK CASP3 CASP7 CASP3/7
  • Product Overview:
    Takinib is a TGF-?-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-?-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-?-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-?-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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