CM-272

CM-272 is a **small molecule dual inhibitor** targeting both **DNA (cytosine-5)-methyltransferase 1 (DNMT1)** and **euchromatic histone-lysine N-methyltransferase 2 (EHMT2, also called G9a)**. It acts as an **epigenetic modulator**, inhibiting the methyltransferase activity of these targets. Mechanistically, CM-272 downregulates G9a and DNMT1 activity, leading to antiproliferative and pro-apoptotic effects in cancer models such as castration-resistant prostate cancer and various solid and hematological malignancies. The drug is being investigated for its anti-tumor effects and potential in combination therapies (e.g., with immune checkpoint inhibitors or cisplatin) in preclinical cancer models, including for kidney fibrosis, prostate cancer, urothelial carcinoma, bile duct neoplasms, and neuroblastoma[1][2][3].