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A-395

CAS No. : 2089148-72-9

MCE 站：A-395

产品活性：A-395 是一种 polycomb 抑制复合物 2 (polycomb repressive complex 2; PRC2) 蛋白质-蛋白质相互作用的拮抗剂，抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12) 的 IC₅₀ 值为 18 nM。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC₅₀ of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 ａnd H3K27me3, with IC₅₀ values of 390 nM ａnd 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.

In Vivo: The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED, with an IC₅₀ of 7 nM. A-395, but not the close chemical analog A-395N, modulates activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 ａnd H3K27me3, with IC₅₀ values of 390 nM ａnd 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.

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