Chaetocin is an epithiodioxopiperazine antibiotic that has recently shown promise as a selective antitumor agent. 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.
Chaetocin is soluble in ethanol, methanol, DMF and DMSO.
Chaetocin is soluble in ethanol, methanol, DMF and DMSO.
| Mechanism of Action | Chaetocin is an inhibitor of lysine-specific methyltransferase SU(VAR)3-9 both in vitro and in vivo. |
| Molecular Formula | C30H28N6O6S4 |
| References | 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. |