LLY-507

Description: LLY-507 is a novel, potent, cell-permeable/active and selective inhibitor of protein-lysine methyltransferase SMYD2 (SET And MYND Domain Containing 2) with an IC50 of 15 nM. SMYD2 is a lysine methyltransferase that catalyzes the monomethylation of several protein substrates including p53. LLY-507 is > 100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets. LLY-507 is active in cells as measured by reduction of SMYD2-induced monomethylation of p53 Lys(370) at submicromolar concentrations. LLY-507 inhibited the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner.

References: LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysineMethyltransferase SMYD2. J Biol Chem. 2015 May 29; 290(22):13641-13653.; Olsen JB, Cao XJ, Han B, Chen LH, Horvath A, Richardson TI, Campbell RM, Garcia BA, Nguyen H. Quantitative Profiling of the Activity of Protein LysineMethyltransferase SMYD2 Using SILAC-Based Proteomics. Mol Cell Proteomics. 2016Mar; 15(3):892-905.