AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal[1].
AZ506 inhibits SMYD2 mediated methylation of monomethyl p53 peptide in U2OS cells with an EC50 of 1.2 μM. AZ506 inhibits SMYD2-mediated methylation (p53-me in U2OS cells) with an IC50 of 2.43 μM[1].
[1]. Cowen SD, et al. Design, Synthesis, and Biological Activity of Substrate Competitive SMYD2 Inhibitors. J Med Chem. 2016;59(24):11079-11097.