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Pifithrin-α 促销  ≥97% (HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(20 mg/mL)
产品描述：基本信息 产品编号：P10054 产品名称：Pifithrin-α CAS: 63208-82-2   储存条件 粉末 -20℃ 四年     分子式： C16H18N2Os.HBr 溶于液体 -80℃ 六个月 分子量 367.30 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 73mg/mL (198.74mM) Ethanol Insoluble Water Insoluble 体内（现配现用） 5% DMSO+ 40% PEG 300+ 5%Tween80+ 50%ddH2O 3.65mg/ml ＜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 2.7226mL 13.6129mL 27.2257mL 5mM 0.5445mL 2.7226mL 5.4451mL 10mM 0.2723mL 1.3613mL 2.7226mL 50mM 0.0545mL 0.2723mL 0.5445mL   生物活性 产品描述 一种p53抑制剂，抑制p53依赖性的p53应答基因转录。 靶点/IC50 p53AhR   体外研究 Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect.Notably,Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates. Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and.Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex,activate reporter activity,and up-regulate the classic AhR target gene CYP1A1. 体内研究 When the experiment is performed with Pifthirin-α (PFT-α) hydrobromide, a pharmacological p53 inhibitor, the percentage of annexin V-positive Foxe3-/- SMCs decreases to WT levels. Pifithrin-α (2.2mg/kg, i.p.) significantly reduces the incidence of aortic rupture and intramural hematomas in Foxe3-/- mice that underwent transverse aortic constriction (TAC) (50% to 17%,P<0.05). After Pifthirin-α treatment, the mean diameter of the ascending aorta and the percentage of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals (P<0.05).   推荐实验方法(仅供参考) 激酶实验： The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25mM Hepes, 1mM EDTA,1mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4mM leupeptin, 4mg/mL aprotinin,and 0.3mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120μg) are incubated at room temperature for 2h with the indicated concentrations of Pifithrin-α in the presence of 3nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice,resuspended in 0.2mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone.   细胞实验:   The human hepatoma cell lines HepG2 (p53++) are cultured in RMPI 1640 medium with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37℃ in an atmosphere containing 5% CO2.Cells are exposed to GOX (0-5 0U) for 0-8 hours with or without Pifithrin-α (20μM/L),Pifithrin-μ (5μM/L), CsA (10μM/L), Sanglifehrin A (20μM/L) and NAC (5mM/L) for 1hour,respectively.After treatment, cells are collected and processed for further experiments.   动物实验:   Mice The Foxe3-null (Foxe3-/-) mice are used. To investigate the role of p53 in Foxe3-related apoptosis,Pifithrin-α is administered by i.p. injection at a dosage of 2.2mg/kg, then dissolved in PBS 1 hour before TAC and then every 48 hours. Animals are euthanized 2 weeks after the surgery, and the ascending aortic tissues are harvested for either RNA, total protein,histomorphometric analysis, or TUNEL assay.
保存条件：-20℃

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