EPZ031686

Description: EPZ-031686 is a potent and selective and orally bioavailable SMYD3 inhibitor with an IC50 of 3 nM in enzymatic/cell-free assay. EPZ031686 shows good bioavailability (F) after oral dosing in mice making it a suitable tool for potential in vivo target validation studies. SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies.

References: NovelOxindole Sulfonamides and Sulfamides: EPZ031686, the First OrallyBioavailable Small Molecule SMYD3 Inhibitor. ACS Med Chem Lett. 2015 Aug27; 7(2):134-8.; Rajajeyabalachandran G, Kumar S, Murugesan T, Ekambaram S, Padmavathy R, Jegatheesan SK, Mullangi R, Rajagopal S. Therapeutical potential of deregulatedlysine methyltransferase SMYD3 as a safe target for novel anticancer agents.Expert Opin Ther Targets. 2017 Feb; 21(2):145-157. doi:10.1080/14728222.2017.1272580. Epub 2016 Dec 26. PubMed PMID: 28019723.