SMYD2 is a lysine N-methyltransferase that methylates both histones and non-histone proteins, including p53 and retinoblastoma-associated protein.{21355,23894} LLY-507 is a cell-active, small molecule inhibitor of SMYD2 (IC50 = 15 nM).{16441} It has been shown to inhibit p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6 µM.{16441} LLY-507 is >100-fold selective for SMYD2 over a panel of 27 protein methyltransferases and non-methyltransferase targets.{16441} See the Structural Genomics Consortium (SGC) website for more information.
产品描述
A selective, cell-active, small molecule inhibitor of SMYD2 (IC50 = 15 nM); inhibits p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6 µM