Product Details
| Product Name:
MS436 |
CAS No.:
1395084-25-9 |
| Purity:
98.92% |
Supply Ability:
10g |
| Release date:
2024/11/13 |
Product Introduction
Bioactivity
| 名稱 | MS436 |
| 描述 | MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains. |
| 細胞實驗 | Murine macrophage RAW264.7 cells are plated at a density of 10000 cells per well in a 96-well plate and incubated at 37 °C for 18 h. The cells are then treated with the diazobenzene bromodomain inhibitors up to 100 μL for 24 hours. At the end of the 24 hr incubation, 10 μL of the MTT solution (4 mg/ml) is added to each well and incubated at 37°C for 4 h. The supernatants are then removed and the cells were solubilized in 100 μL of 100% DMSO. The diazobenzene compounds are first dissolved in DMSO then diluted with culture medium to concentrations that ranged from 0.28 to 50000 nM. The final concentration of DMSO is adjusted to 0.05% (v/v). The extent of the reduction is measured by the absorbance at 570/630 nm using EnVison 2104 Multilabel Reader.(Only for Reference) |
| 激酶實驗 | Fluorescence Anisotropy Binding Assay: Binding affinity of the newly synthesized diazobenzene compounds for various bromodoamins is assessed in a fluorescence anisotropy competition assay using a fluorescein isothiocyanate (FITC)-labeled MS417 as an assay probe. Competition experiments are performed with a BrD protein (0.25–1 μM) and the fluorescent probe (80 nM), and increasing concentration of unlabeled competing ligand in a PBS buffer (pH 7.4) in total volume of 80 μL Measurements are obtained after a 1 hour incubation of the fluorescent ligand and the protein at 25°C with Safire 2 microplate reader. In a competition-binding assay, fluorescent ligand concentration is ≤ 2Kd, and protein concentration was set at which 50-80% of fluorescent ligand is bound. Dissociation constant of a competing ligand is calculated with the correction to Cheng-Prussoff equation introduced by Nicolovska-Coleska and colleagues. Assuming one-site competitive binding model, the equation used to calculate Ki's from IC50 values recovered from fitting data using Prism. |
| 體內活性 | MS436 exhibits low nanomolar affinity (Ki=30-50 nM) for the first bromodomain of BRD4. In mouse macrophages with NF-κB-directed expression, MS436 inhibits BRD4 activity, reducing the levels of NO and IL-6. |
| 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 : 40 mg/mL (104.32 mM)
|
| 關鍵字 | Inhibitor | MS436 | inhibit | Epigenetic Reader Domain | MS 436 | MS-436 |
| 相關產品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
| 相關庫 | 組蛋白修飾化合物庫 | 細胞重編程化合物庫 | 表型篩選靶點鑒定庫 | 經典已知活性庫 | 表觀遺傳庫 | 自噬庫 | 染色質修飾分子庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
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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Recommended supplier
| Product name |
Price |
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Suppliers |
Update time |
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$1.00/1KG |
VIP7Y
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Career Henan Chemical Co
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2019-09-03 |
United States