CAY10657

The NF-κB/Rel family of transcription factors induce and coordinate the expression of pro-inflammatory genes including cytokines, chemokines, interferons, MHC proteins, growth factors, and cell adhesion molecules. Under resting conditions NF-κB dimers are retained in the cytoplasm by a member of the IKB family of inhibitory proteins. Upon activation by cytokines or other stimuli, IKK phosphorylates IKB, initiating a signaling cascade to activate gene transcription. CAY10657 is a thiophenecarboximide derivative proposed to inhibit IKK2. Currently, there are no published reports of its biological activity. However, inhibition of NF-κB activation is likely to be of broad utility in the treatment of inflammatory diseases and cancer.