CM-2303

CM-2303 is a potent and selective small molecule inhibitor of the histone methyltransferases **G9a** (EHMT2) and **GLP** (EHMT1). Developed by the Center for Applied Medical Research (CIMA) at the University of Navarra, it targets the epigenetic regulation of gene expression by preventing the dimethylation of histone H3 lysine 9 (H3K9me2), a mark associated with transcriptional silencing. CM-2303 has demonstrated significant anti-proliferative activity in various cancer models, particularly in hematological malignancies such as acute myeloid leukemia (AML) and B-cell lymphomas, as well as certain solid tumors. By inhibiting G9a/GLP, the compound induces the re-expression of tumor suppressor genes and promotes cell cycle arrest and apoptosis. It serves as a precursor or related scaffold to the dual G9a/DNMT inhibitor CM-272, which is also part of CIMA's epigenetic drug discovery program.