p-nitro-Cyclic Pifithrin-α
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
p-nitro-Cyclic Pifithrin-α is an inactivator of p53.
The activation of the tumor suppressor gene p53 plays a key role in regulating the in-vitro death of neurons, following apoptotic stimuli molecules including glutamate and DNA-damaging agents. Thus, p53 inhibitors may prove effective in suppressing the degenerative processes in neurodegenerative disorders.
In vitro: Pifithrin-α (PFT-α) was identified as an inactivator of p53 blocking p53-dependent transcriptional activation and apoptosis. Cyclic PFT-α was a stable analog of PFT-α. p-nitro-Cyclic PFT-α, a cell-permeable form of cyclic PFT-α, was found to be one order of magnitude more active than PFT-α in protecting cortical neurons exposed to etoposide. p-nitro-Cyclic PFT-α acted in a p53-dependently but did not block phosphorylation of p53 on Ser15 in response to etoposide treatment, although it prevented p53 posttranscriptional activity [1].
In vivo: In a previou study, C57BL/6 mice were fed a high-fat (HFD) or control diet for 8 weeks; PFT was administered three times per week. Results showed that PFT administration could suppress HFD-induced weight gain, steatosis, oxidative stress, ALT elevation, and apoptosis. PFT treatment also able to blunt the HFD-induced upregulation of miRNA34a and increase SIRT1 expression. In the livers of HFD-fed, PFT-treated mice, activation of the SIRT1/PGC1α/PPARα axis increased the expression of malonyl-CoA decarboxylase [2].
Clinical trial: So far, no clinical study has been conducted.
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. Journal of Medicinal Chemistry 49(12), 3645-3652 (2006).
[2] Derdak Z, Villegas KA, Harb R, Wu AM, Sousa A, Wands JR. Inhibition of p53 attenuates steatosis and liver injury in a mouse model of non-alcoholic fatty liver disease. J Hepatol. 2013 Apr;58(4):785-91.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 299.3 |
Cas No. | 60477-38-5 |
Formula | C15H13N3O2S |
Synonyms | Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α |
Solubility | ≤1mg/ml in dimethyl formamide |
Chemical Name | 5,6,7,8-tetrahydro-2-(4-nitrophenyl)-imidazo[2,1-b]benzothiazole |
SDF | Download SDF |
Canonical SMILES | O=[N+](C(C=C1)=CC=C1C2=CN(C(S3)=N2)C4=C3CCCC4)[O-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |