Chaetocin is a fungal mycotoxin, originally produced by Chaetomium species, that inhibits the lysine-specific histone methyltransferases (HMTs) SU(VAR)3-9 (IC50 = 0.8 μM)
HMTs are responsible for methylation of histones, thereby affecting heterochromatinization
Chaetocin is also known to inhibit G9a and DIM5 (IC50 = 2.5 μM and 3 μM respectively; Cherblanc et al.; Greiner et al.) Chaetocin also acts as a competitive substrate and inhibitor of the central oxidative stress remediation enzyme thioredoxin reductase-1 (TrxR1; Km = 4.6 μM) more potently than glutathione reductase or thioredoxin (Tibodeau et al.)
Induces cellular oxidative stress, selectively killing cancer cells and rapidly-proliferating primary cells (Isham et al.; Spannhoff et al.)
Attenuates the growth of glioma xenografts accompanied by an increase in reactive oxygen species (ROS) production (Dixit et al.)
