BRD9539
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货号：A535666
BRD9539 inhibits G9a activity with an IC50 of 6.3 μM, inhibits PRC2 activity with a similar IC50.
BRD9539 化学结构
BRD9539 3D分子结构
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BRD9539 纯度/质量文件 产品仅供科研
货号：A535666
标准纯度：
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产品说明书
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BRD9539 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, IC50: 11 nM
EZH2, Ki: 2.5 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
98%
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, Ki: 0.33 nM
SETD7, IC50: 2 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 nM
99%+
BIX-01294 3HCl
+
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
BRD9539 生物活性
靶点
描述
The methylation of lysine 9 on histone H3 by the histone methyltransferase G9a is a modification related to aberrant silencing of tumor suppressor genes. BRD9539 is the potential active form of BRD4770, a histone methyltransferase inhibitor in cells. BRD9539 dose-dependently inhibited G9a activity with an IC50 value of 6.3μM, but its inhibitory effect decreased with increasing S -adenosylmethionine concentrations. BRD9539 also blocked PRC2 activity with a similar IC50 value but had no inhibitory effect against SUV39H1 or DNMT1 up to 40μM. BRD9539 showed no activity in cell-based assays, probably due to impaired cell permeability. BRD9539 at 5 or 10μM exhibited no inhibitory activity towards 100 kinases related to cell-cycle regulation and cancer cell biology, and 16 other chromatin-modifying enzymes[1]
BRD9539 参考文献
[1] Yuan Y, Wang Q, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.
[2] Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp MM, Adams DJ, Shamji AF, Wagner BK, Schreiber SL. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7
BRD9539 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.50mL
0.50mL
0.25mL
12.52mL
2.50mL
1.25mL
25.03mL
5.01mL
2.50mL
BRD9539 技术信息
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