中文名称:

BRD9539

中文同义词:

G9A和PRC2抑制剂(BRD9539)

英文名称:

BRD-9539

英文同义词:

BRD 9539;BRD9539;BRD-9539;2-(BenzoylaMino)-1-(3-phenylpropyl)-1H-benziMidazole-5-carboxylic acid;1H-Benzimidazole-5-carboxylic acid, 2-(benzoylamino)-1-(3-phenylpropyl)-

CAS号:

1374601-41-8

分子式:

C24H21N3O3

分子量:

399.44

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1374601-41-8.mol

储存条件 

2-8°C

溶解度 

DMSO: soluble15mg/mL, clear

形态

powder

颜色

white to beige

生物活性

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。

靶点

G9a 6.3 μM (IC 50 ) PRC2

G9a 6.3 μM (IC 50 )

PRC2

体外研究

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.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3