Histone Methyltransferase
Histone methyltransferases (HMT) are histone-modifying enzymes), that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. Methylation of histones is important biologically because it is the principal epigenetic modification of chromatin that determines gene expression, genomic stability, stem cell maturation, cell lineage development, genetic imprinting, DNA methylation, and cell mitosis.
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EPZ-6438是一种有效的，选择性EZH2抑制剂，Ki为2.5 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。
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BIX 01294是一种G9ahistone methyltransferase（组蛋白甲基转移酶）抑制剂，IC50为2.7 μM，降低组蛋白H3K9me2，也能微弱抑制GLP（主要是H3K9me3），对其他组蛋白甲基转移酶没有显著的抑制活性。
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SGC0946是组蛋白甲基转移酶DOT1L高效选择性抑制剂，IC50值为0.3nM,有效抑制混合系白血病细胞。
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MI-3是Menin-MLL相互作用抑制剂，IC50为648 nM。
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UNC 0631是G9a抑制剂，IC50为4nM。
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