I-CBP112 NEW
| Price | $29 | $48 | $98 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: I-CBP112 | CAS No.: 1640282-31-0 |
| Purity: 99.1% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | I-CBP112 |
| 描述 | I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains. |
| 細(xì)胞實驗 | 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]. |
| 激酶實驗 | 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 |
| 體外活性 | Exposure to I-CBP112 in human and mouse leukemic cell lines significantly reduces colony formation and initiates cellular differentiation, without notable cytotoxic effects. When primary cells from the BioMAP panel were treated with I-CBP112, it elicited a distinctive cytokine and marker protein expression profile. Importantly, I-CBP112 markedly increases acetylation levels at histone H3K18 and H3K23 sites by p300, tripling H3K18ac levels. This compound not only enhances CBP-mediated acetylation at these locations but also at H4K5. The half-maximal effective concentration (EC50) for I-CBP112's action on p300 and CBP to increase H3K18 acetylation is approximately 2 μM. |
| 體內(nèi)活性 | I-CBP112 markedly diminishes the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner [both in vitro and in vivo]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (117.37 mM) |
| 關(guān)鍵字 | I-CBP112 | Inhibitor | HATs | I CBP112 | inhibit | I-CBP 112 | HAT | ICBP112 | I-CBP-112 | Epigenetic Reader Domain | Histone Acetyltransferase |
| 相關(guān)產(chǎn)品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Acetaminophen | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin |
| 相關(guān)庫 | 細(xì)胞重編程化合物庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 染色質(zhì)修飾分子庫 | 血液病分子庫 | 抑制劑庫 | NO PAINS 化合物庫 | PPI抑制劑庫 | 已知活性化合物庫 | 抗高血壓化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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