Drug intelligence / Profile preview

AZ506

Development stage
Discontinued
Lead developer
Gladstone Institutes
Modality
Small Molecules
01

Overview

AZ506 is a potent, selective, research-grade small-molecule inhibitor of the protein lysine methyltransferase SMYD2, with an in vitro IC50 of approximately 17 nM against SMYD2 enzymatic activity.[1][4][10] By blocking SMYD2-mediated lysine methylation of substrates such as the tumor suppressor p53, AZ506 modulates oncogenic signaling and epigenetic regulation and is used as a chemical probe to study SMYD2 biology in cancer and other diseases.[1][4] Preclinical work has also used AZ506, alongside other SMYD2 inhibitors, to downregulate TMPRSS2 expression and reduce SARS-CoV-2 replication in cell culture, highlighting potential antiviral relevance at the target level, though AZ506 itself is not developed as a therapeutic drug.[9]

Other names
AZ-506AZ506AZ 506
02

Targets

SMYD2

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