CPI-17

CPI-17 is a small molecule transcriptional inhibitor of the CYP24A1 gene, which encodes the primary enzyme responsible for the degradation of the active form of vitamin D, 1,25-dihydroxyvitamin D3 (1,25D3). Identified by researchers at the Roswell Park Cancer Institute through a high-throughput screen of the DIVERSet library, CPI-17 was found to significantly inhibit 1,25D3-induced CYP24A1 promoter activity and subsequent mRNA and protein expression in various cancer cell lines, including prostate, bladder, and kidney cancer. By reducing the local inactivation of vitamin D within the tumor microenvironment, CPI-17 is intended to enhance the anti-proliferative and pro-apoptotic effects of 1,25D3, potentially overcoming a major mechanism of resistance to vitamin D-based therapies in oncology.