A TAK1 inhibitor (IC50 = 9.5 nM); selective for TAK1 over IRAK1

Takinib – 5 mg

Brand:
Cayman
CAS:
1111556-37-6
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 24161 - 5 mg Category:

Description

A TAK1 inhibitor (IC50 = 9.5 nM); selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively); increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells; reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells; inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes; reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis at 50 mg/kg per day

Formal name: N1-(1-propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide

Synonyms: 

Molecular weight: 322.4

CAS: 1111556-37-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis

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