Histone Demethylase
There are several families of histone demethylases, which act on different substrates and play different roles in cellular function. Histone demethylases are a diverse group of enzymes catalyzing a process to reverse histone methylation, in which methyl (CH3-) groups are removed from instead of being transferred to histone. A code has been developed to indicate the substrate for a histone demethylase. The substrate is first specified by the histone subunit (H1, H2A, H2B, H3, H4) and then the one letter designation and number of the amino acid that is methylated. Lastly, the level of methylation is sometimes noted by the addition of "me#", with the numbers being 1, 2, and 3 for monomethylated, dimethylated, and trimethylated substrates, respectively. For example, H3K9me2 is histone H3 with a dimethylated lysine in the ninth position.
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SP2509是组蛋白去甲基化酶LSD1新型抑制剂,IC50值为13nM,对MAO-A和MAO-B基本无抑制作用。
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Tranylcypromine hydrochloride is a racemic mixture of (±)-Trans-2-phenylcyclopropyl-1-amine (TCP, tPCPA) · HCl that covalently inhibits the LSD and MAO enzymes. Tranylcypromine (2-PCPA) HCl是一种非选择性的不可逆的单胺氧化酶(MAO)抑制剂,用作抗抑郁药和抗焦虑药。
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ML324是JMJD2去甲基酶抑制剂,被证实有抗病毒作用。
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GSK-J1是一个高效和选择性的H3K27去甲基化酶抑制剂,体外对人源JMJD3的IC50值为60 nM。
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