| CAS NO: | 389850-21-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 398.3 |
| Cas No. | 389850-21-9 |
| Formula | C15H15N3O3S·HBr |
| Synonyms | p-nitro-PFT-α |
| Solubility | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide |
| Chemical Name | 1-(4-nitrophenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)-ethanone, monohydrobromide |
| Canonical SMILES | N=C(S1)N(CC(C2=CC=C([N+]([O-])=O)C=C2)=O)C3=C1CCCC3.Br |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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