h4r3me2a

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.

PRMT1-IN-3 is a potent inhibitor of protein arginine methyltransferase 1 (PRMT1) with an IC50 of 4.11 μM. It also inhibits PRMT6 and PRMT8, with IC50 values of 23.3 and 30.1 μM, respectively. In triple-negative breast cancer (TNBC) cells, PRMT1-IN-3 reduces asymmetric dimethylarginine (ADMA) levels and the histone modification H4R3me2a. It induces cell cycle arrest and apoptosis in MDA-MB-231 cells and inhibits cell migration and colony formation. Furthermore, PRMT1-IN-3 serves as a chemosensitizer for Paclitaxel and is applicable in TNBC research.