Cot inhibitor-1

Description: Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer. Target: MAPK, TNF. Smiles: Fc1ccc(Nc2c(cnc3c(Cl)cc(NCc4cn(CCN5CCCCCC5)nn4)cc23)C#N)cc1Cl. References: Wu J, et al. Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. Bioorg Med Chem Lett. 2009,19(13):3485-3488.