MC3817 is a selective DNMT inhibitor, with IC50 values of 0.044 μM for DNMT1 and greater than 10 μM for DNMT3A/3L. It inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage, and elevates the levels of cleaved Caspase 3, P53, and γH2AX. MC3817 is applicable in research on non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer, and histiocytic lymphoma.

DNMT1:0.044 μM

MC3817 (compound 14) demonstrates anticancer activity against various cell lines, including A549 and H460 (non-small cell lung cancer and lung cancer cells), HCT-116 (colon cancer), HeLa (cervical cancer), MDA-MB-231 (triple-negative breast cancer), and U937 (histiocytoma lymphoma) at concentrations ranging from 0.05 to 100 μM over a period of 48 hours. At 2 μM, MC3817 causes cell cycle arrest at the S/G2M phase and induces apoptotic cell death in HCT-116 cells over 24 to 48 hours. Within the range of 0.5 to 5 μM over 16 to 48 hours, MC3817 triggers DNA damage and activates the p53/γH2AX pathway, leading to cell cycle arrest and apoptosis in HCT-116 cells. Additionally, at 2.5 μM over 48 hours, MC3817 induces apoptosis in HCT-116 P53 WT cells at levels significantly higher than those induced in HCT-116 P53 −/− cells.