Pifithrin-α, p-Nitro, Cyclic

Modify Date: 2024-01-20 09:56:07

Pifithrin-α, p-Nitro, Cyclic Structure
Pifithrin-α, p-Nitro, Cyclic structure
Common Name Pifithrin-α, p-Nitro, Cyclic
CAS Number 60477-38-5 Molecular Weight 299.348
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C15H13N3O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Pifithrin-α, p-Nitro, Cyclic


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].

 Names

Name 2-(4-Nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
Synonym More Synonyms

 Pifithrin-α, p-Nitro, Cyclic 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
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

 Synonyms

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