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CPI-11 is a small molecule transcriptional inhibitor of CYP24A1, the primary enzyme responsible for the degradation of 1á,25-dihydroxyvitamin D3 (1,25D3). Identified through a high-throughput screen of the DIVERSet™ library by researchers at the Roswell Park Cancer Institute, CPI-11 was selected for its ability to inhibit 1,25D3-induced CYP24A1 promoter activity. By reducing the expression of CYP24A1, CPI-11 aims to prevent the rapid local inactivation of vitamin D in tumor environments, thereby potentially enhancing the anti-proliferative and pro-apoptotic effects of 1,25D3 in various cancers, including prostate, bladder, and kidney cancer.
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