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NF-κB-IN-5 (compound 4d) is an orally active NF-κB inhibitor. NF-κB-IN-5 interacts directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines, with IC 50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, PC9, respectively.