Chaetocin is an inhibitor of histone methyltransferases (HMTs) including SUV39H1 and Lys9-specific HMTs such as G9a. It also has some inhibitory effects on SET7, EZH2, and SET7/9. Chaetocin can also induce cellular oxidative stress, selectively killing cancer cells and rapidly-proliferating primary cells. It is a fungal myotoxin. The inhibitor is useful in epigenetics and cancer research.

≥95% by HPLC

Chaetocin inhibits SUV39H1 with an IC50 = 0.8 µM, G9a with an IC50 = 2.5 µM , and DIM5 with an IC50 = 3 µM .

Soluble in organic solvents purged with an inert gas and solubility is 25 mg/ml.

A crystalline solid.

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

1. Greiner, D., et al., Nat. Chem. Biol. 2005;1(3):143-145.
2. Isham, C.R., et al., Blood 2007;109(6):2579-2588.
3. Tibodeau, J.D., et al., Antioxid. Redox Signal. 2009;11(5):1097-1106.

Methyltransferase

Inhibitor