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EPZ005687

CAS No. : 1396772-26-1

MCE 站：EPZ005687

产品活性：EPZ005687 是一种有效的，选择性的 EZH2 抑制剂，K_i 值为 24 nM，对其选择性是对 EZH1 的 50 倍，对其他 15 种甲基转移酶的 500 倍。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: EPZ005687 shows concentration-dependent inhibition of PRC2 enzymatic activity with an IC₅₀?value of 54±5 nM. EPZ005687 specifically inhibits H3K27 methylation in lymphoma cells. EPZ005687 has a notable effect on proliferation of the EZH2Y641F-bearing cell line. EPZ005687 decreases proliferation in mutant but not wild-type EZH2 lymphoma cells. EPZ005687 (0.5, 1, 5 and 10 ?M) induces an obvious apoptosis of U937 cells in a dose-dependent manner. EPZ005687 inhibits obviously the proliferation of U937 cells but has weak effect on the proliferation of NBMCD34⁺ cells. EPZ005687 induces G1 phase blocking and decreases the percentage of cells in S phase in U937 cells. In addition, EPZ005687 produces obviously depletion of H3K27 methylation in U937 cells, but hardly has effect on the H3K27 methylation of NBMCD34⁺ cells.

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