中文名称:

PRT4165

中文同义词:

2-(3-吡啶亚甲基)-1,3-茚满二酮;H2A泛素化抑制剂(PRT4165);化合物PRT 4165

英文名称:

NSC 600157

英文同义词:

PRT 4165; PRT-4165; NSC600157; NSC-600157; NSC 600157;2-(pyridin-3-ylmethylidene)indene-1,3-dione;2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione;2-(3-Pyridylmethylene)-1,3-indandione;NSC 600157;PRT4165;PRT 4165(NSC 600157);1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)-

CAS号:

31083-55-3

分子式:

C15H9NO2

分子量:

235.24

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

31083-55-3.mol

沸点 

377.63°C (rough estimate)

密度 

1.1757 (rough estimate)

折射率 

1.6231 (estimate)

储存条件 

2-8°C

溶解度 

DMSO: soluble20mg/mL, clear

形态

powder

颜色

white to beige

生物活性

PRT4165 是一种有效的 PRC1 介导的 H2A 泛素化的抑制剂。

靶点

PRC1

体外研究

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation. In vitro E3 ubiquitin ligase activity assays reveal that PRT4165 inhibits both RNF2 and RING 1A, but not RNF8 nor RNF168. In the presence of PRT4165, H2A ubiquitylation can be completely inhibited regardless of whether RING1 or RNF2 contributes the E3 ubiquitin ligase activity. Treatment of cells for 60 min with 50 μM PRT4165 results in a dramatic reduction in total ubiquitylated histone H2A. It is also found that longer exposure of the cells with the PRT4165 (30 and 60 min) leads to increased levels of γ-H2AX in unirradiated cells. PRT4165 inhibits double-strand break (DSB) repair at the 8-h time point compare with mock treated cells. Cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G 2 /M.

WGK Germany 

3

RTECS号

NK6710000