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化学名
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(3S,3'S,6R,6'R,14R,14'R,16S,16'S)-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-2,2',3,3',6,6',7,7'-octahydro-1H,1'H-[14,14'-bi(3,11a-epidithiopyrazino[1',2':1,5]pyrrolo[2,3-b]indole)]-1,1',4,4'(15H,15'H)-tetraone
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分子式
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C30H28N6O6S4
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详细内容
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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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