OTS193320 is an inhibitor of SUV39H2 methyltransferase activity. OTS193320 reduces global histone H3 lysine 9 trimethylation levels and triggers apoptosis in breast cancer cells. The combination of OTS193320 and Doxorubicin reduced γ-H2AX levels and cancer cell viability compared to OTS193320 or Doxorubicin alone. In the concentration range of 0.125-0.5 μM for 24 h, OTS193320 showed growth inhibitory effect on breast cancer cell lines. OTS193320 showed high inhibitory effect on SUV39H2 enzyme activity (IC50=22.2 nM) and growth inhibitory effect on SUV39H2 positive A549 lung cancer cells (IC50=0.38 μM). At a concentration of 0.5 μM for 48 hours, OTS193320 induced apoptosis in breast cancer cells. In the concentration range of 0.125-0.5 μM for 24 hours, OTS193320 reduced H3K9me3 levels in a dose-dependent manner[1].
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