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Cmp3 (Compound 3) is a small molecule antagonist of the nuclear receptor subfamily 5 group A member 2 (NR5A2), also known as liver receptor homolog-1 (LRH-1). NR5A2 is a key transcription factor involved in the regulation of cholesterol metabolism, bile acid synthesis, and cellular proliferation. In the context of oncology, particularly colorectal cancer (CRC), NR5A2 has been identified as a driver of cancer stem cell (CSC) stemness and tumor progression. Cmp3 functions by binding to the ligand-binding domain of NR5A2, thereby inhibiting its transcriptional activity and downregulating downstream targets such as the stemness-related transcription factor NANOG. Research indicates that treatment with Cmp3 can reduce the stem-like properties of CRC cells, inhibit cell proliferation, and suppress tumor growth in preclinical models, making it a valuable chemical probe for studying NR5A2-mediated signaling pathways.
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