BRD9 bromodomain inhibitor

BRD9 bromodomain inhibitors are a class of small molecule epigenetic modulators that selectively target the bromodomain of Bromodomain-containing protein 9 (BRD9), a key subunit of the non-canonical BAF (ncBAF) SWI/SNF chromatin remodeling complex. By binding to the acetyl-lysine recognition pocket of the BRD9 bromodomain, these inhibitors prevent the protein from reading histone modifications, thereby disrupting the recruitment of the SWI/SNF complex to specific genomic loci, such as the MYC enhancer. This disruption leads to the suppression of oncogenic transcriptional programs and has shown preclinical efficacy in models of acute myeloid leukemia (AML), synovial sarcoma, and other malignancies where BRD9 is essential for cell proliferation and maintenance of an undifferentiated state. Notable chemical probes in this class include I-BRD9, BI-7273, BI-9564, and GNE-375.

Other names

BRD9 inhibitorsBRD-9 inhibitorsBRD 9 inhibitors