BAY-184

BAY-184 is a selective small molecule inhibitor of the lysine acetyltransferases KAT6A and KAT6B. It belongs to a novel class of acylsulfonamide-benzofuran compounds identified through high-throughput screening and refined via computational modeling and co-crystallization studies. KAT6A and KAT6B are epigenetic regulators that catalyze the transfer of acetyl groups to histone proteins, thereby influencing chromatin structure and gene expression. Amplification of the KAT6A gene, particularly within the 8p11-p12 chromosomal region, is observed in approximately 12-15% of breast cancer cases and is associated with increased expression of chromatin-modifying enzymes. BAY-184 has demonstrated in vivo efficacy in proof-of-concept studies, suggesting its potential as a targeted therapy for cancers characterized by KAT6A/B dysregulation. The compound was developed through a collaboration involving Bayer Pharma AG, Nuvisan ICB GmbH, and the Broad Institute.