Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 273 | 现货 | ||
2 mg | ¥ 388 | 现货 | ||
5 mg | ¥ 628 | 现货 | ||
10 mg | ¥ 843 | 现货 | ||
25 mg | ¥ 1,680 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,090 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 628 | 现货 |
产品描述 | Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes. |
体外活性 | 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. |
体内活性 | 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。 |
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[2]. |
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) |
别名 | Pifithrin hydrobromide, Pifithrin-α (PFTα) HBr, Pifithrin-α, PFTα, PFTα hydrobromide |
分子量 | 367.3 |
分子式 | C16H18N2OS·HBr |
CAS No. | 63208-82-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 36.7 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7226 mL | 13.6129 mL | 27.2257 mL | 68.0643 mL |
5 mM | 0.5445 mL | 2.7226 mL | 5.4451 mL | 13.6129 mL | |
10 mM | 0.2723 mL | 1.3613 mL | 2.7226 mL | 6.8064 mL | |
20 mM | 0.1361 mL | 0.6806 mL | 1.3613 mL | 3.4032 mL | |
50 mM | 0.0545 mL | 0.2723 mL | 0.5445 mL | 1.3613 mL | |
100 mM | 0.0272 mL | 0.1361 mL | 0.2723 mL | 0.6806 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Pifithrin-α hydrobromide 63208-82-2 Apoptosis Immunology/Inflammation Ferroptosis Aryl Hydrocarbon Receptor p53 inhibit Pifithrin-a (PFTa) HBr Pifithrin α hydrobromide Inhibitor MDM-2/p53 Pifithrin-alpha PFTa Hydrobromide Pifithrin-alpha Hydrobromide Pifithrin-a AhR Pifithrin Pifithrin hydrobromide PFTalpha Hydrobromide Pifithrin-α (PFTα) HBr Pifithrin Hydrobromide PFTalpha Pifithrin-α Pifithrin-a Hydrobromide PFTα Pifithrin-alpha (PFTalpha) HBr Pifithrinα hydrobromide PFTα Hydrobromide Pifithrin-α Hydrobromide PFTα hydrobromide PFTa inhibitor