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AZ505, a molecule identified from a high throughput chemical screen, is a potent and selective inhibitor of SET and MYND domain-containing 2 protein (SMYD2), a protein lysine methyltransferase catalyzing the methylation of both histone (H2B, H3 and H4) and non-histone protein substrates including the tumor suppressor proteins p53 and Rb, with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 0.12 μM and 0.3 μM respectively [1].

AZ505 has been found to be a substrate competitive inhibitor of SMYD2, where it binds into the peptide binding groove of SMYD2 competing with the peptide substrates rather than the co-factor [1].

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