Fig. 1
Novel TNF-R1 inhibitors demonstrate target engagement by blocking TNF-R1 signaling pathways. a Molecular structures of experimental compounds (C7 and SGT11) differ at R1 (C7 = OAc, SGT11 = OH), R2 = CF3. b C7 and SGT11 were tested to inhibit the TNFα-induced luciferase reporter gene expression controlled by NF-κB promoter. The percentage of inhibition of TNFα-induced reporter gene expression is shown. c Inhibition of TNF-α-induced phosphorylation of IκB in murine fibroblast L929 cells. The cells were pretreated with inhibitors for 1 h and stimulated by human TNFα at 5 ng/ml for 5 min. Phosphorylation and total protein levels of IκB and p38 were examined by western blot. The data represent a typical result derived from several experiments