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• 产品描述： BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1

• 靶点： G9a:6.3 μM (IC50);PRC2;HistoneMethyltransferase

• 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.

• 参考文献：
  1. Yuan, Y., Wang, Q., Paulk, J., et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma ACS Chem. Biol. 7(7), 1152-1157 (2012).

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.503 ml	12.517 ml	25.035 ml
  5 mM	0.501 ml	2.503 ml	5.007 ml
  10 mM	0.25 ml	1.252 ml	2.503 ml
  50 mM	0.05 ml	0.25 ml	0.501 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *