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p-nitro-Cyclic Pifithrin-α

Catalog No.
C5104
inactivator of p53
Grouped product items
SizePriceStock Qty
5mg
$137.00
Ship with 5-10 days
10mg
$252.00
Ship with 5-10 days
25mg
$533.00
Ship with 5-10 days

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Email: [email protected]

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Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt299.3
Cas No.60477-38-5
FormulaC15H13N3O2S
SynonymsCyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α
Solubility≤1mg/ml in dimethyl formamide
Chemical Name5,6,7,8-tetrahydro-2-(4-nitrophenyl)-imidazo[2,1-b]benzothiazole
SDFDownload SDF
Canonical SMILESO=[N+](C(C=C1)=CC=C1C2=CN(C(S3)=N2)C4=C3CCCC4)[O-]
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

p-nitro-Cyclic Pifithrin-α