LLY-507 is a potent, selective and cell-active inhibitor of SMYD2 (IC50<15 nM).
LLY-507 displays >100-fold selective over a broad range of methyltransferase and non-methyltransferase targets.
LLY-507 inhibits SMYD2-mediated methylation of p53 Lys370 and suppresses proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner (IC50=1.5-6 uM).
