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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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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PFI-2是甲基转移酶SETD7高效选择性抑制剂,IC50值为2nM。
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MI-2 (Menin-MLL Inhibitor)是一种有效的menin-MLL相互作用抑制剂,IC50为446 nM。
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UNC0379是一个选择性、底物竞争性SETD8赖氨酸甲基转移酶抑制剂,IC50值为7.3±1.0uM,对其他15种甲基转移酶有很好的选择性。
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