Powder: -20°C for 3 years | In solvent: -80°C for 1 year
I-CBP112 是一种特异性的乙酰赖氨酸竞争性蛋白质-蛋白质相互作用抑制剂,靶向 CBP/p300 溴结构域,增强 p300 的乙酰化作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 819 | 现货 | ||
2 mg | ¥ 1,190 | 现货 | ||
5 mg | ¥ 2,290 | 现货 | ||
10 mg | ¥ 3,390 | 现货 | ||
25 mg | ¥ 5,460 | 现货 | ||
50 mg | ¥ 7,430 | 现货 | ||
100 mg | ¥ 9,830 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,380 | 现货 |
产品描述 | I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains. |
靶点活性 | CBP-p300 (Prostate cancer cells):9.1±1.2 μM (IC50), CBP-p300 (Leukemia cells):5.5±1.1 μM (IC50) |
体外活性 | Exposure of human and mouse leukemic cell lines to I-CBP112 results in substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. Exposure of the BioMAP primary cell panel to I-CBP112 results in a unique response on cytokine and marker protein expression. I-CBP112 significantly enhances acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, I-CBP112 induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC50's of activation of I-CBP112 on p300- and CBP-mediated H3K18 acetylation are ~2 μM. |
体内活性 | I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner in vitro and in vivo. |
激酶实验 | TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2 |
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[1]. |
分子量 | 468.59 |
分子式 | C27H36N2O5 |
CAS No. | 1640282-31-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (117.37 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1341 mL | 10.6703 mL | 21.3406 mL | 53.3515 mL |
5 mM | 0.4268 mL | 2.1341 mL | 4.2681 mL | 10.6703 mL | |
10 mM | 0.2134 mL | 1.067 mL | 2.1341 mL | 5.3352 mL | |
20 mM | 0.1067 mL | 0.5335 mL | 1.067 mL | 2.6676 mL | |
50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.067 mL | |
100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5335 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
I-CBP112 1640282-31-0 Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase Inhibitor HATs I CBP112 inhibit I-CBP 112 HAT ICBP112 I-CBP-112 inhibitor