PKC-ι inhibitor

PKC-ι (Protein Kinase C-iota) inhibitors are a class of targeted therapies designed to inhibit the activity of the atypical protein kinase C isoform iota. PKC-ι is an oncogene frequently overexpressed in various cancers, including prostate cancer, melanoma, ovarian cancer, and glioblastoma, where it promotes cell survival, proliferation, and epithelial-mesenchymal transition (EMT). Research, particularly from the University of South Florida, has identified PKC-ι as a regulator of the NF-κB pathway and a key player in avoiding senescence. Experimental inhibitors such as ICA-1 and gold compounds like aurothiomalate have been studied for their ability to selectively target the PB1 domain or the catalytic domain of PKC-ι, thereby inducing apoptosis and reducing tumor growth in preclinical models. These inhibitors have also been shown to downregulate the expression of PKC-ι itself, suggesting a self-regulatory mechanism that can be exploited for therapeutic benefit.

Other names

PKC-iota inhibitorProtein kinase C-iota inhibitorPRKCI inhibitor