Chemical Name: 4-Methyl-3-[[6-(methylamino)-4-pyrimidinyl]oxy]-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]benzamide
Biological ActivityPotent MAP4K2 (GCK) inhibitor (IC50 = 37 nM). Exhibits >70-fold selectivity for MAP4K2 over TAK1 (IC50 = 2.7 μM for TAK1). Inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation, in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
Tan et al.
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