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BRD9539

CAS No. : 1374601-41-8

MCE 站：BRD9539

产品活性：BRD9539 是一种组蛋白甲基转移酶 G9a 抑制剂，IC₅₀ 为 6.3 μM。BRD9539 还抑制 PRC2 活性，并且对 SUV39H1，NSD2 和 DNMT1 无活性。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: BRD9539 decreases ATP levels in a dose-dependent manner in HeLa cells.
BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. However, BRD9539 has no activity in cell-based assays, presumably due to impaired cell permeability compared to that of BRD4770. In addition, the activities of 16 other chromatin-modifying enzymes and 100 kinases involved in cell-cycle regulation and cancer cell biology are tested for activity in the presence of 5 or 10 μM BRD9539; no activity is seen in any of these assays.

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