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BRD4770 is a small molecule inhibitor of the histone methyltransferase G9a (also known as EHMT2). It was structurally derived from BIX-01338 and acts by reducing the di- and trimethylation of lysine 9 on histone H3 (H3K9). Primarily used as a research tool, BRD4770 has demonstrated preclinical activity in inducing senescence in pancreatic cancer cells and protecting against doxorubicin-induced cardiotoxicity by inhibiting cardiomyocyte ferroptosis and apoptosis. It has also been investigated for its potential to enhance NK cell-mediated anti-tumor immunity through the suppression of TGF-β1. The compound is not currently approved for human use and is not being developed by a specific pharmaceutical company for a therapeutic indication.
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