| 名稱 | Pifithrin-α hydrobromide |
| 描述 | Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes. |
| 細胞實驗 | 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) |
| 激酶實驗 | 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]. |
| 體外活性 | 10 μM Pifithrin-α抑制Dox,Etoposide,Taxol和Cytosine arabinoside誘導(dǎo)的C8細胞凋亡。10 μM Pifithrin-α降低熱休克轉(zhuǎn)錄因子的激活,且增強細胞對熱的敏感性。10 μM Pifithrin-α降低HeLa細胞中糖皮質(zhì)激素受體的激活,且保護小鼠胸腺免受Dexamethasone誘導(dǎo)的凋亡。100–200 nM Pifithrin-α完全抑制海馬細胞中Camptothecin誘導(dǎo)的p53 DNA結(jié)合水平和p53應(yīng)答基因Bax的增加。200 nM Pifithrin-α保護培養(yǎng)的海馬神經(jīng)元免受DNA損傷劑誘導(dǎo)的死亡。200 μM Pifithrin-α穩(wěn)定線粒體功能,抑制caspase活化,保護培養(yǎng)的海馬神經(jīng)元免受谷氨酸和β-淀粉樣肽誘導(dǎo)的死亡。 Pifithrin-α抑制人類二倍體成纖維細胞對DNA損傷的p53依賴性生長抑制,但對p53缺陷型成纖維細胞沒有影響。Pifithrin-α可調(diào)節(jié)p53的核輸入或輸出（或兩者同時）,也可降低核p53的穩(wěn)定性。Pifithrin-α可以抑制熱休克和糖皮質(zhì)激素受體信號,但不影響NF-κB信號。 |
| 體內(nèi)活性 | 小鼠腹腔注射3.6 μg/kg Pifithrin-α,抑制Dex誘導(dǎo)的胸腺退化.Pifithrinα（2 mg/kg）與對照組相比,在大腦中動脈暫時閉塞的大鼠中導(dǎo)致運動障礙程度顯著降低.在小鼠大腦中動脈閉塞治療前30分鐘,Pifithrin-α（2 mg/kg i.p.）減少缺血性腦損傷并保護海馬神經(jīng)元免受興奮毒性損傷.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射線照射造成的損傷.通過Tunel和caspase 3染色,觀察到 Pifithrin-α明顯降低大鼠的細胞凋亡.當(dāng)在中風(fēng)發(fā)作后一小時內(nèi)施用藥物時,Pifithrinα處理的動物具有較少的運動障礙和較小的梗塞.與空白對照組相比,Pifithrin-α處理7天后,明顯降低大鼠的運動障礙評分 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 36.7 mg/mL (100 mM)
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| 關(guān)鍵字 | inhibit | Pifithrin-a (PFTa) HBr | Ferroptosis | Pifithrin α hydrobromide | Inhibitor | Aryl Hydrocarbon Receptor | MDM-2/p53 | Pifithrin-alpha | PFTa Hydrobromide | Pifithrin-alpha Hydrobromide | Pifithrin-a | AhR | Pifithrin | PFTalpha Hydrobromide | Pifithrin Hydrobromide | PFTalpha | Pifithrin-a Hydrobromide | Pifithrin-alpha (PFTalpha) HBr | Pifithrinα hydrobromide | PFTα Hydrobromide | Pifithrin-α Hydrobromide | PFTa |
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