MS2928

**MS2928** is a small molecule inhibitor of SETD8 (also known as KMT5A), a histone methyltransferase that catalyzes monomethylation of histone H4 at lysine 20 (H4K20me1), an epigenetic modification associated with DNA repair, cell cycle progression, and cancer cell proliferation. It demonstrates superior potency in reducing H4K20me levels compared to the tool compound UNC0379. In preclinical studies, MS2928 selectively inhibits the growth of multiple myeloma (MM) cells with high SETD8 expression, while sparing SETD8-low MM cells, suggesting potential utility as a targeted therapy for SETD8-overexpressing malignancies.[1][2]