Potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC50
= 50 nM). Selective for Tpl2 over MEK, p38, Src, MK2, PKC and EGFR. Inhibits LPS-induced TNF-α
secretion from monocytes and attenuates acute myeloid leukemia (AML) cell proliferation in vitro
. Also reduces cytolytic activity of human CD8+
cytotoxic T lymphocytes. Cell permeable.
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All Tocris products are intended for laboratory research use only.
Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions.
Chowdhury et al.
PLoS ONE, 2014;9:e92187
Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3.
Wang et al.
Cell Cycle, 2010;9:4542
Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Gavrin et al.