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• 产品描述： GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

• 靶点： IC50: 4 nM (EZH2), 240 nM (EZH1);HistoneMethyltransferase; Autophagy

• 体内研究：
  Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels

• 参考文献：
  1. Sharad K, et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. 2. Ding M, et al. The polycomb group protein enhancer of zeste 2 is a novel therapeutic target for cervical cancer. Clin Exp Pharmacol Physiol. 2015 May;42(5):458-64.

• 溶解性： DMSO  :  15.62  mg/mL  (28.84  mM;  Need  ultrasonic)    H2O  :  <  0.1  mg/mL  (ultrasonic;warming;heat  to  60°C)  (insoluble)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.846 ml	9.23 ml	18.461 ml
  5 mM	0.369 ml	1.846 ml	3.692 ml
  10 mM	0.185 ml	0.923 ml	1.846 ml
  50 mM	0.037 ml	0.185 ml	0.369 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。

• 1. [IF=3.7] Yun Zhang et al."MAPRE3 as an epigenetic target of EZH2 restricts ovarian cancer proliferation in vitro and in vivo."EXPERIMENTAL CELL RESEARCH.2024 Jan;:113913

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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 *