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Nanaomycin A is a naturally-derived small molecule antibiotic and the first selective inhibitor of DNA methyltransferase 3B (DNMT3B), exhibiting an IC50 of approximately 500 nM. As a quinone antibiotic, it downregulates DNA methylation and reactivates silenced tumor suppressor genes by demethylating their promoters, notably RASSF1A, making it a promising epigenetic modulator for cancer research. Nanaomycin A shows antiproliferative effects on various human cancer cell lines and induces apoptosis in neuroblastoma cells, indicating a therapeutic potential for cancer, particularly neuroblastoma and other DNMT3B-driven tumors[1][3][4][8].
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