Key Points Nuclear factor of κB (NF-κB) is a transcriptional regulator that is made up of different protein dimers that bind a common sequence motif known as the κB site. Although NF-κB target genes have been most intensely studied for their involvement in immunity and inflammation, this transcription factor also regulates cell proliferation, apoptosis and cell migration. Therefore, it is not surprising that NF-κB has been shown to be constitutively activated in several types of cancer cell. NF-κB activity is tightly controlled by several regulatory proteins, and disruption of this process has been associated with various haematological malignancies, as well as epithelial tumours such as breast cancer. A causal connection between inflammation and cancer has been suspected for many years. Because NF-κB becomes activated in response to inflammatory stimuli and its constitutive activation has been associated with cancer, NF-κB might also serve as the missing link between these two processes. Numerous inhibitors of NF-κB are therefore under development or have been developed. Because of the widespread importance of this factor, it has been difficult to develop NF-κB inhibitors that act specifically in cancer cells. Learning more about the complicated process of NF-κB regulation should lead to better therapeutic approaches to target the factor in specific cell types.