Chaetocin is an epithiodioxopiperazine antibiotic that has recently shown promise as a selective antitumor agent. Chaetocin is a specific inhibitor for the lysine-specific methyltransferase SU(VAR)3-9 both in vitro and in vivo. Chaetocin is dramatically accumulated in cancer cells via a process inhibited by glutathione. Inside the cell, its activity is mediated by the imposition of oxidative stress.
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