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MS436  ≥98%(HPLC)

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溶解性：溶于DMSO(25mg/mL 超声 加热)
产品描述：基本信息 产品编号：M10321 产品名称：MS436 CAS: 1395084-25-9   储存条件 粉末 -20℃ 四年     分子式： C18H17N5O3S 溶于液体 -80℃ 六个月 分子量： 383.43 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 55mg/mL (143.44mM) Ethanol 1mg/mL warmed with 50ºC water bath (2.6mM) Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6081mL 13.0405mL 26.0811mL 5mM 0.5216mL 2.6081mL 5.2162mL 10mM 0.2608mL 1.3041mL 2.6081mL 50mM 0.0522mL 0.2608mL 0.5216mL   生物活性 产品描述 一种BRD4抑制剂。 靶点/IC50 BRD4 (1)  BRD4 (2) <0.085μM(Ki) 0.34μM(Ki)   体外研究 MS436,through a set of water-mediated interactions,exhibits low nanomolar affinity (estimated Ki of 30-50nM) with preference for the first bromodomain over the second.MS436 effectively inhibits BRD4 activity in NF-κB-directed production of NO and pro-inflammatory cytokine interleukin-6 in murine macrophages.MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.MS436 exhibits potent affinity of an estimated Ki=30-50nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2,which is achieved through a unique set of water-mediated intermolecular interactions.   推荐实验方法(仅供参考) 激酶实验： Binding affinity of the newly synthesized diazobenzene compounds (e.g.,MS436) 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 (0.25-1µM) and the fluorescent probe (80nM),and increasing concentration of unlabeled competing ligand in a PBS buffer (pH 7.4) in total volume of 80µL Measurements are obtained after a 1 hour incubation of the fluorescent ligand and the protein at 25℃ with Safire 2 microplate reader.In a competitionbinding assay,fluorescent ligand concentration is≤2Kd,and protein concentration is 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.   细胞实验:   Murine macrophage RAW264.7 cells are plated at a density of 1×104 cells per well in a 96-well plate and incubated at 37℃ for 18h.The cells are then treated with the diazobenzene bromodomain inhibitors (e.g.,MS436) up to 100µM for 24 hours.At the end of the 24hr incubation,10µL of the MTT solution (4mg/mL) is added to each well and incubated at 37℃ for 4h.The supernatants are then removed and the cells are solubilized in 100µL of 100% DMSO.The diazobenzene compounds are first dissolved in DMSO then diluted with culture medium to concentrations that ranged from 0.28 to 50000nM.The final concentration of DMSO is adjusted to 0.05% (v/v).The extent of the reduction is measured by the absorbance at 570/630nm using EnVison 2104 Multilabel Reader
保存条件：-20℃

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