Powder: -20°C for 3 years | In solvent: -80°C for 2 years
M344 是一种组蛋白去乙酰化酶抑制剂，IC50为 100 nM。
| 产品描述 | M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation. |
| 靶点活性 | HDAC:100 nM |
| 体内活性 | 在体外,M344显示出对子宫内膜癌细胞系Ishikawa和卵巢癌细胞系SK-OV-3的显著抗增殖活性,EC50分别为2.3 μM和5.1 μM。而正常的人子宫内膜上皮细胞对M344几乎不敏感。高于10 μM浓度时的M344具有毒性,而最多只有20%的存活细胞群被诱导分化。此外,M344也会导致细胞周期中S期细胞比例减少,G0/G1期细胞比例增加,诱导细胞凋亡,并降低线粒体的跨膜电位。 |
| 激酶实验 | Enzyme Inhibition : Radioactively labeled chicken core histones are used as the enzyme substrate. The enzyme liberated tritiated acetic acid from the substrate which is quantitated by scintillation counting. IC50 values are results of triple determinations. 50 μL of maize enzyme (at 30 °C) is incubated (30 minutes) with 10 μL of total [3H]acetate-prelabeled chicken reticulocyte histones (1 mg/mL). Reaction is stopped by addition of 36 μL of 1 M HCl/0.4 M acetate and 800 μL of ethyl acetate. After centrifugation (10000 g, 5 minutes) an aliquot of 600 μL of the upper phase is counted for radioactivity in 3 mL of liquid scintillation cocktail. M344 is tested in a starting concentration of 40 μM, and active substances are diluted further. |
| 细胞实验 | MEL DS19 cells (murine erythroleukemia cells) are maintained in D-MEM containing 100 units/mL penicillin G sodium and 100 μg/mL streptomycin sulfate supplemented with 10% fetal bovine serum at 37 °C in a 5% CO2 atmosphere. To test M344 for potential to induce cell differentiation, log-phase cells with a population doubling time of 11−13 hours are used. Serial dilutions of M344 are prepared in 24-well plates using 1 mL of D-MEM/well. If M344 are dissolved in DMSO, control wells contains the same amount of solvent (generally 2 μL/mL of medium). Subsequently, the cell suspension is added to the wells. After 72 hours the experiment is evaluated. Cell numbers are counted using a Casy 1 TTC flow cytometer. The proliferation of treated cells is expressed as percent proliferation in comparison with the solvent control. Differentiated MEL cells accumulate hemoglobin. Therefore, the induction of cell differentiation is determined by benzidine staining according to the literature. To 100 μL of cell suspension is added 10 μL of a 0.4% solution of benzidine in 12% acetic acid containing 2% Water2. Within 5 minutes hemoglobin-containing cells stains blue. Benzidine-positive and -negative cells are counted under the microscope in a hemocytometer, and the percentage of positive cells is calculated. M344 is first tested at 10 μM and 50 μM final concentration. According to activity/toxicity profile, a range of concentrations is chosen for a dose−response analysis. (Only for Reference) |
| 别名 | Histone Deacetylase Inhibitor III, MS 344 |
| 分子量 | 307.39 |
| 分子式 | C16H25N3O3 |
| CAS No. | 251456-60-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Ethanol: 4 mg/mL (13.01 mM)
H2O: <1 mg/mL
DMSO: 62 mg/mL (201.69 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多...
体内实验配液计算器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。
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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。
M344 251456-60-7 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibit M 344 Inhibitor Histone Deacetylase Inhibitor III D-237 MS-344 MS 344 D237 MS344 D 237 M-344 Histone deacetylases inhibitor
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