OTS193320

OTS193320 is a potent, small-molecule inhibitor of the histone methyltransferase SUV39H2 (Suppressor of variegation 3-9 homolog 2), also known as KMT1B. Developed by OncoTherapy Science in collaboration with the University of Chicago, the compound selectively targets SUV39H2, which is highly expressed in various cancers (such as breast and lung cancers) and plays a key role in heterochromatin maintenance, DNA repair, and chemoresistance. OTS193320 decreases global histone H3 lysine 9 tri-methylation (H3K9me3) levels, triggers apoptotic cell death, and downregulates γ-H2AX production. When combined with doxorubicin, OTS193320 sensitizes breast cancer cells to chemotherapy by attenuating DNA repair pathways. It has been evaluated in preclinical models of breast and lung cancers.