Chaetocin is an epithiodioxopiperazine antibiotic that has recently shown promise as a selective antitumor agent. Chaetocin is an inhibitor of 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.
- Isolation and configuration of Chaetocin. Hauser, D. et al., Helv. Chim. Acta 1970, 53, 1061.
- Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Greiner D. et al., Nature Chem. Biol. 2005, 1, 143.
- Chaetocin, a promising new anti-myeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Isham C.R. et al., Blood 2007, 109, 2579.