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化學性質:
規格 | 1mg 5mg 10mg 25mg |
CAS | 389850-21-9 |
別名 | p-nitro-PFT-α |
化學名 | 1-(4-nitrophenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)-ethanone, monohydrobromide |
分子式 | C15H15N3O3S ? HBr |
分子量 | 398.3 |
溶解度 | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
p-nitro-Pifithrin-α, a cell-permeable cyclic analog of pifithrin-α, is an inhibitor of p53 activity [1].
The p53 tumor suppressor gene product can induce apoptotic cell death and plays a dominant role in apoptosis, genomic stability, and inhibition of angiogenesis. The p53 has been considered to be an oncogene and the wild-type gene product actually functions as a tumour suppressor gene. p53 mutations play an important role in the development of many common human malignancies [2].
In Vitro: In p53-/- cortical neuron, p-nitro-Pifithrin-α exihibited a p53 inhibitory activity in preventing p53-induced death[1]. p-nitro-Pifithrin-α did not prevent cortical neuronal death induced by p40Met, showing the remarkable specificity in the inhibitory action of p-nitro-Pifithrin-α on p53. p-nitro-Pifithrin-α (300 nM) prevented p53-triggered increase in protein levels of p21/WAF1, indicating that p-nitro-Pifithrin-α behaved as p53 posttranscriptional activity inhibitors. p-nitro-Pifithrin-α at a dose of 30 nM was sufficient to prevent the increase of p21/WAF1 levels [1]. p-nitro-Pifithrin-α was slowly converted into a more potent cyclized form, p-nitro cyclic pifithrin-α, when incubated in biological media (t1/2= 8 h)
In human proximal tubular cells, p-nitro-Pifithrin-α (10 μM) suppressed p53-mediated TGF-β1 expression [3].
In vivo: In a mouse model of non-alcoholic fatty liver disease, p-nitro-Pifithrin-α attenuated steatosis and liver injury in mice fed a high-fat diet [4].
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原創作者:上海莼試生物技術有限公司
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賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278