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• 产品描述： GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM

• 靶点： IC50: 80 nM (BRPF1);EpigeneticReaderDomain

• 体外研究：
  GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold). GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay. GSK-5959 has no effect on TRIM24 SUMOylation

• 参考文献：
  1. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195. 2. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71. 3. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.535 ml	12.675 ml	25.351 ml
  5 mM	0.507 ml	2.535 ml	5.07 ml
  10 mM	0.254 ml	1.268 ml	2.535 ml
  50 mM	0.051 ml	0.254 ml	0.507 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *