Six new 2,4-linked exo/endo sesquiterpene lactone dimers, faberidilactones A–E (1–5) and endodischkuhriolin (6), were isolated from Carpesium faberi. The characteristic chemical shift of Ha-3′ and diagnostic negative/positive CE can be used to assign the exo/endo stereochemistry of those dimers. Compounds 1–3, 5 and 6 exhibited potent cytotoxicity with IC₅₀ value in the range of 1.11–8.50 μM against the four human tumor cell lines (CCRF-CEM, K562, HL-60 and HCT116 cells). Moreover, 1, 3 and 5 (exo-SLDs) showed potent NF-κB inhibitory effect with inhibition ratio of 65.98, 53.27 and 71.45%, respectively.