Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers[2].IC50 & Target:Tpl2/COT kinase/MAP3K8In Vitro:Tpl2 (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family that is upstream of MEK in the ERK pathway.
Tpl2 Kinase Inhibitor 1 (compound 2p) also inhibits MK2 and p38, with IC50s of 110 μM and 180 μM, respectively in A431 cells.
Tpl2 Kinase Inhibitor 1 inhibits lipopolysaccharide-induced TNF-a production from primary human monocytes and human whole-blood, with IC50s of 0.7 μM and 8.5 μM, respectively.
Cancer Osaka thyroid (COT) kinase (Tpl2) is an important regulator of pro-inflammatory cytokines in macrophages[2].