• 产品描述： UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).

• 靶点： GLP:<2.5 nM, G9a:<2.5 nM;HistoneMethyltransferase

• 体外研究：
  UNC0642 (Ki: 3.7±1 nM) is competitive with the peptide substrate and non-competitive with the cofactor SAM. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, transporters, GPCRs, and ion channels. UNC0642 exhibits high potency at low cell toxicity, reducing the H3K9me2 mark, and good separation of functional potency in a number of cell lines

• 体内研究：
  UNC0642 (5 mg/kg, i.p.) results in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/ml.

• 细胞实验： MDA-MB-231, PC3, and U2OS cells are treated with UNC0642 for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm

• 动物实验： Mouse: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following UNC0642 (5 mg/kg, i.p.). The compound concentration at each time point in plasma or brain is the average value from 3 test animals

• 参考文献：
  1. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.829 ml	9.146 ml	18.292 ml
  5 mM	0.366 ml	1.829 ml	3.658 ml
  10 mM	0.183 ml	0.915 ml	1.829 ml
  50 mM	0.037 ml	0.183 ml	0.366 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。

输入产品批号：

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 *