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SJ018 is a selective small molecule inhibitor of the second bromodomain (BD2) of the Bromodomain and Extra-Terminal (BET) family of proteins. Developed by researchers at St. Jude Children's Research Hospital, SJ018 is designed to target the epigenetic regulation of gene transcription. In preclinical models of pancreatic ductal adenocarcinoma (PDAC), SJ018 has demonstrated superior potency compared to pan-BET inhibitors like I-BET762. Its mechanism involves suppressing cell proliferation, inducing DNA damage (marked by increased γH2AX), and inhibiting the expression of the homologous recombination repair protein Rad51. By specifically targeting the BD2 domain, SJ018 aims to provide a more targeted therapeutic approach with potentially improved efficacy and safety profiles over non-selective BET inhibitors.
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