2245255-66-5

GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM[1][2].

SMYD3: 14 nM (Ki); SMYD3: 130 nM (IC₅₀)

[1] Van Aller GS, et al. Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets. Structure. 2016 May 3;24(5):774-781. DOI:10.1016/j.str.2016.03.010
[2] Kaniskan Hü, et al. Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev. 2018 Feb 14;118(3):989-1068. DOI:10.1021/acs.chemrev.6b00801