化学性质：                                                                                                             

产品描述：                                                                                                             

Chaetocin, a natural thiodioxopiperazine product from Chaetomium species, is a lysine-specific histone methyltransferase inhibitor, which reduces the histone methyltransferase effects of SUV39H1 with IC50 value of 0.8 μM.

SUV39H1 is a histone methyltransferase that can methylate Lys-9 of histone H3 and plays an important role in many processes including repression of MYOD1-stimulated differentiation, regulation of the cell cycle and celll differentiation, and regulation of telomere length.

Chaetocin was found to have apoptotic effects on some cancer cells. In patient CD138+ myeloma cells, chaetocin has the potent antimyeloma activity which is attributable to reactive oxygen species (ROS) induction imposed by inhibition of the redox enzyme thioredoxin reductase [1].  Chaetocin reduced the methylation of H3K9 and H3K27 in HL-60 and KG-1a cells [2].

The component has also been used in animal models to study the role of SUV39H1. This component exhibits anti-proliferative activity and anti-cancer effect in a mouse myeloma xenografts model [3].

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