KTX-1001, also referred to as NSD2 inhibitor 161, is an innovative and potent inhibitor of nuclear SET domain-containing protein 2 (NSD2). This compound specifically binds to NSD2, inhibiting its catalytic activity and the mono- and dimethylation of histone H3 lysine 36 (H3K36). Such regulation impacts gene expression involved in cellular processes, including proliferation, which may subsequently slow cancer cell growth. NSD2 is part of the NSD family of histone lysine methyltransferases, which are often overexpressed and dysregulated in various cancer types.