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p-nitro-Pifithrin-α
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
p-nitro-Pifithrin-α图片
CAS NO:389850-21-9
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
p-nitro-Pifithrin-α，一种 pifithrin-α 的细胞渗透类似物，是一种有效的 p53 抑制剂。
Cas No.389850-21-9
别名p-nitro-PFT-α
化学名1-(4-nitrophenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)-ethanone, monohydrobromide
Canonical SMILESN=C(S1)N(CC(C2=CC=C([N+]([O-])=O)C=C2)=O)C3=C1CCCC3.Br
分子式C15H15N3O3S o HBr
分子量398.3
溶解度≤1mg/ml in DMSO;1mg/ml in dimethyl formamide
储存条件Store at -20°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[1] Pietrancosta N, Moumen A, Dono R, et al.  Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism[J]. Journal of medicinal chemistry, 2006, 49(12): 3645-3652.
[2] Nigro J M, Baker S J, Preisinger A C, et al.  Mutations in the p53 gene occur in diverse human tumour types[J]. Nature, 1989, 342(6250): 705-708.
[3] Shimizu H, Yisireyili M, Nishijima F, et al.  Indoxyl sulfate enhances p53-TGF-β1-Smad3 pathway in proximal tubular cells[J]. American journal of nephrology, 2013, 37(2): 97-103.
[4] Derdak Z, Villegas K A, Harb R, et al.  Inhibition of p53 attenuates steatosis and liver injury in a mouse model of non-alcoholic fatty liver disease[J]. Journal of hepatology, 2013, 58(4): 785-791.