Cancer is one of the most common diseases in the world. Th e transcription factor NF-κB plays a key role in various physiological processes including immune response, cell proliferation, cell apoptosis and inflammation. Due to participation of NF-kappa B signaling pathways in carcinogenesis, angiogenesis, and tumor resistance to chemo- and radiotherapy, the factor is considered to be the ideal target for pharmacological treatment of cancer. Th e paper presents a literature review of the RSCI, PubMed, Scopus, Web of Science, Chemical Abstracts NCCN databases and other open access data. The carcinogenesis inhibitors were selected from all NF-κB inhibitors found. Inhibitors with antitumor activity of analytical interest include Bruton tyrosine kinase (BTK) inhibitors, cellular inhibitors of apoptosis proteins (c-IAP), proteasome inhibitors, and one inhibitor of NF-κB translocation to the nucleus. Th e authors analyzed products of diff erent development stages with recorded antitumor activity to varying degrees. NF-κB inhibitors are promising drug candidates, but since NF-κB is involved in most biological processes and the broad spectrum of action can cause side eff ects, the selective action of these compounds is to be explored.