A-83-01
3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole
Transforming Growth Factor-b Type I Receptor Kinase Inhibitor IV Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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-b receptors. Inhibits TGF-b-induced Smad2-phosphorylation in HaCaT cells and epithelial-to-mesenchymal transition in NMuMG cells at a concentration of 1 µM. Purity: ≥98% by HPLC. Ref.: Tojo, M., et al. 2005. Cancer Sci. 96, 791. |
