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FX1 is a potent, selective, small-molecule inhibitor of B-cell lymphoma 6 (BCL6) that targets the BTB domain lateral groove. Developed through in silico drug design (SILCS) by researchers at Weill Cornell Medicine and the University of Maryland, FX1 binds to the BCL6 BTB domain with high affinity, disrupting its interaction with corepressors such as SMRT, NCOR, and BCOR. This disruption reactivates BCL6 target genes and suppresses BCL6-dependent cancers, particularly diffuse large B-cell lymphoma (DLBCL) and triple-negative breast cancer (TNBC). FX1 has also demonstrated anti-inflammatory properties in models of sepsis, inflammatory bowel disease (IBD), and lymphoid hyperplasia, as well as the ability to repress HIV infection in follicular helper T (Tfh) cells.
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