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Pifithrin-α hydrobromide(98.17%)  Cite:0    分享

货号: LK-62538
复制产品信息
  • CAS:63208-82-2
  • 分子式:C16H18N2OS·HBr
  • 分子量:367.3
  • 纯度:98.17%
  • 用途:p53抑制剂
规格:
1MG 5MG 10MG 25MG 50MG 100MG 1 mL x 10 mM (in DMSO)
单位:
单价:¥453.00
化学信息
生物信息
溶解度信息
储存与保存
注意事项
化学信息
  • 产品名称
    Pifithrin-α hydrobromide
  • 别名
    Pifithrin-α (PFTα) HBr, Pifithrin-α, Pifithrin hydrobromide, PFTα hydrobromide, PFTα
  • CAS
    63208-82-2
  • 分子式
    C16H18N2OS·HBr
  • 分子量
    367.3
  • Smiles
    Br.Cc1ccc(cc1)C(=O)Cn1c2CCCCc2sc1=N
  • 密度
    1.28g/cm3
  • 颜色
    白色
生物信息
  • 产品描述
    Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) 是一种 p53 抑制剂,可抑制 p53 反应基因的 p53 依赖性反式激活。它也是芳烃受体的激动剂
  • Targets(IC50)
    Apoptosis,Ferroptosis,Aryl Hydrocarbon Receptor,p53,MDM-2/p53
  • 体外活性
    10 μM Pifithrin-α抑制Dox,Etoposide,Taxol和Cytosine arabinoside诱导的C8细胞凋亡。10 μM Pifithrin-α降低热休克转录因子的激活,且增强细胞对热的敏感性。10 μM Pifithrin-α降低HeLa细胞中糖皮质激素受体的激活,且保护小鼠胸腺免受Dexamethasone诱导的凋亡。100–200 nM Pifithrin-α完全抑制海马细胞中Camptothecin诱导的p53 DNA结合水平和p53应答基因Bax的增加。200 nM Pifithrin-α保护培养的海马神经元免受DNA损伤剂诱导的死亡。200 μM Pifithrin-α稳定线粒体功能,抑制caspase活化,保护培养的海马神经元免受谷氨酸和β-淀粉样肽诱导的死亡。 Pifithrin-α抑制人类二倍体成纤维细胞对DNA损伤的p53依赖性生长抑制,但对p53缺陷型成纤维细胞没有影响。Pifithrin-α可调节p53的核输入或输出(或两者同时),也可降低核p53的稳定性。Pifithrin-α可以抑制热休克和糖皮质激素受体信号,但不影响NF-κB信号
  • 体内活性
    小鼠腹腔注射3.6 μg/kg Pifithrin-α,抑制Dex诱导的胸腺退化.Pifithrinα(2 mg/kg)与对照组相比,在大脑中动脉暂时闭塞的大鼠中导致运动障碍程度显著降低.在小鼠大脑中动脉闭塞治疗前30分钟,Pifithrin-α(2 mg/kg i.p.)减少缺血性脑损伤并保护海马神经元免受兴奋毒性损伤.C57BL和Balb/c小鼠腹腔注射2.2 mg/kg Pifithrin-α,使小鼠完全免受60%致死率的γ射线照射造成的损伤.通过Tunel和caspase 3染色,观察到 Pifithrin-α明显降低大鼠的细胞凋亡.当在中风发作后一小时内施用药物时,Pifithrinα处理的动物具有较少的运动障碍和较小的梗塞.与空白对照组相比,Pifithrin-α处理7天后,明显降低大鼠的运动障碍评分
  • 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 [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [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 0.2 mL 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
    At the end of cell treatments, the number of attached cells is estimated by staining with 0.25% crystal violet in 50% methanol, followed by elution of the dye with 1% SDS. Optical density (530 nm) reflecting the number of stained cells is determined with a Bio-Tek EL311 microplate reader. Cell viability in suspension of short term culture of primary thymocytes is determined by their staining with 0.1% of methyl blue and microscopic counting of blue (dead) cells.(Only for Reference)
溶解度信息

■ Solubility
DMSO: 50 mg/mL (136.13 mM),Sonication is recommended.
(< 1 mg/ml refers to the product slightly soluble or insoluble)
■ In vivo Formulation 
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.45 mM),Sonication isrecommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one.Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared andused immediately. The formulation provided above is for reference purposes only. In vivo formulations mayvary and should be modified based on specific experimental conditions.
■ Preparing Stock Solutions


1mg5mg10mg
  1 mM2.7226 mL13.6129 mL27.2257 mL
  5 mM0.5445 mL2.7226 mL5.4451 mL
  10 mM0.2723 mL1.3613 mL2.7226 mL
  50 mM0.0545 mL 0.2723 mL 0.5445 mL

Please select the appropriate solvent to prepare the stock solution, according to the solubility of the product indifferent solvents. Please use it as soon as possible.
Note: The dilution table applies only to solid products. For liquid products, please calculate the stock solution basedon the stated concentration and/or density.

储存与保存

1. Powder: -20°C for 3 years 
2. In solvent: -80°C for 1 year
keep away from direct sunlight
实际储存温度以产品标签为准

注意事项

1. 我司生产的生化试剂如无特殊标注,基本为非无菌包装,若用于细胞实验,请提前做好预处理。需低温保存的产品,一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
2. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

3. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

4. 实验结果可由多种因素影响,相关处理只限于产品本身,不涉及其他赔偿。

 

备注:由于产品信息可能会有优化升级。请以实际收货标签信息为准。

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