A new compound, kalopanaxin F (3), and 11 known compounds (1, 2, 4-12), were isolated from the stem bark of Kalopanax pictus. Their structures were elucidated on the basis of chemical and spectroscopic methods. Five of the compounds (2, 3, 5, 6, and 12) significantly inhibited $TNF{alpha}$-induced NF-${kappa}B$ transcriptional activity in HepG2 cells in a dose-dependent manner, with $IC_{50}$ values ranging from 6.2 to 9.1 ${mu}M$. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 3-7, 9, and 12 significantly activated the transcriptional activity of PPARs dose-dependently, with $EC_{50}$ values ranging from 4.1-$12.7{mu}M$. Compounds 4 and 5 exhibited $PPAR{alpha}$, $PPAR{gamma}$, and $PPAR{eta}({delta})$ transactivational activities in a dose-dependent manner, with $EC_{50}$ values of 16.0 and 17.0, 8.7 and 16.5, 26.2 and 26.3 ${mu}M$, respectively.