BRD9539

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Chemical Structure| 1374601-41-8 同义名 : -
CAS号 : 1374601-41-8
货号 : A535666
分子式 : C24H21N3O3
纯度 : 98%
分子量 : 399.44
MDL号 : MFCD23704793
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(40.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • bromodomain
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.04mL

5.01mL

2.50mL
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