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Beschreibung

A cell-permeable trisubstituted pyrazole compound that has been shown to selectively inhibit ALK-4/5/7-mediated (IC50 = 45, 12, and 7.5 nM, respectively, in luciferase transcription activity assays), but not ALK-1/2/3/6-mediated cellular signaling in Mv1Lu R4-2 transfectants expressing the individual Type I TGF-beta receptors. Inhibits TGF-beta-induced Smad2-phosphorylation in HaCaT cells and epithelial-to-mesenchymal transition in NMuMG cells at a concentration of 1 µ,M.