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• 产品描述： I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.

• 靶点： Epigenetic Reader Domain;Histone Acetyltransferase;EpigeneticReaderDomain; HistoneAcetyltransferase

• 体内研究：
  I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner in vitro and in vivo.

• 细胞实验： I-CBP112 is dissolved in DMSO and diluted with appropriate medium before use. Cells (6000 KG1a and 13000 LNCaP cells/well) are plated in 96-well flat-bottom plates approximately 24 h prior to drug treatment. After 24 h, 10–20% fetal bovine serum-containing medium is replaced with 2.5% serum medium, and cells are treated with I-CBP112 in 0.18% DMSO; 0.18% DMSO is shown to have negligible cell growth effects under the conditions used in our experiments. After being exposed to I-CBP112 for 66 h, cells are subjected to a final concentration of 0.476% [3H]thymidine per well and allowed to proliferate for an additional 6 h (exposure to I-CBP112 for a total of 72 h). Cells are harvested, and the counts of 3H in each well are taken relative to those treated with vehicle alone to quantify the effect of the ligand on proliferation

• 参考文献：
  1. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19. 2. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃;干燥

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.134 ml	10.67 ml	21.341 ml
  5 mM	0.427 ml	2.134 ml	4.268 ml
  10 mM	0.213 ml	1.067 ml	2.134 ml
  50 mM	0.043 ml	0.213 ml	0.427 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 *