LLY-507

LLY-507 is a potent, cell-permeable, small molecule inhibitor of SMYD2 (IC₅₀ = 15 nM), a lysine N-methyltransferase.  It has been shown to inhibit p53 lysine monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC₅₀ value of 0.6 µM. LLY-507 is >100-fold selective for SMYD2 over a panel of 27 protein methyltransferases and non-methyltransferase targets.