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Product Name:p-nitro-Pifithrin-α
CAS:389850-21-9
Purity:>=95% Remarks:Reach out to us for more information about custom solutions.
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Pifithrin-α, p-Nitro manufacturers
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| | Pifithrin-α, p-Nitro Basic information |
| Product Name: | Pifithrin-α, p-Nitro | | Synonyms: | Pifithrin-α, p-Nitro;p-nitro-Pifithrin-α;2-(2-IMINO-4,5,6,7-TETRAHYDROBENZO[D]THIAZOL-3(2H)-YL)-1-(4-NITROPHENYL)ETHANONE HBR;p-nitro-Pifithrin-.alpha.;2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-nitrophenyl)ethanone;Pifithrin-alpha, p-Nitro hydrobromide,;p-Nitropifithrin-alpha, p53 inhibitor | | CAS: | 389850-21-9 | | MF: | C15H16BrN3O3S | | MW: | 398.27484 | | EINECS: | | | Product Categories: | | | Mol File: | 389850-21-9.mol |  |
| | Pifithrin-α, p-Nitro Chemical Properties |
| Melting point | 239-240 °C(Solv: methanol (67-56-1); ethyl acetate (141-78-6)) | | storage temp. | Store at -20°C, protect from light | | solubility | Soluble in DMSO or ethanol | | form | Solid | | color | White to light yellow | | Sensitive | Light Sensitive & Hygroscopic |
| | Pifithrin-α, p-Nitro Usage And Synthesis |
| Uses | A cell-permeable p53 inhibitor | | Biological Activity | 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 human proximal tubular cells, p-nitro-pifithrin-α (10 μm) suppressed p53-mediated tgf-β1 expression [3]. | | 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 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]. | | IC 50 | Caspase-3 | | 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. |
| | Pifithrin-α, p-Nitro Preparation Products And Raw materials |
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