Pifithrin-α, p-Nitro, Cyclic

Names

[ Name ]:
Pifithrin-α, p-Nitro, Cyclic

[Synonym ]:
2-(4-Nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
Imidazo[2,1-b]benzothiazole, 5,6,7,8-tetrahydro-2-(4-nitrophenyl)-
MFCD05670249

Biological Activity

[Description]:

Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> MDM-2/p53

Research Areas >> Neurological Disease

[In Vitro]

Pifithrin-α, p-Nitro, Cyclic (PFN-α) efficiently blocks p53-triggered cell death and p21/WAF1 expression in cortical neurons exposed to etoposide at concentrations one order magnitude lower than that in PFT-α[1].

[In Vivo]

Intraocular injection of pifithrin-α slightly increases survival of retinal ganglion cell (RGC) at the concentration of 6 μM but not at 0.06 μM. Pifithrin-α, p-Nitro, Cyclic (PFN-α) is not effective in vivo, even at 6 μM[1]. Pifithrin-α, p-Nitro, Cyclic shows the half-life (t1/2) of 6 hours (when incubated in biological conditions)[1].

[References]

[1]. Pietrancosta N, et al. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism. J Med Chem. 2006 Jun 15;49(12):3645-52.

[2]. Dinca EB, et al. p53 Small-molecule inhibitor enhances temozolomide cytotoxic activity against intracranial glioblastoma xenografts. Cancer Res. 2008 Dec 15;68(24):10034-9.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₁₅H₁₃N₃O₂S

[ Molecular Weight ]:
299.348

[ Exact Mass ]:
299.072845

[ LogP ]:
5.63

[ Index of Refraction ]:
1.780

Related Compounds

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