Pifithrin-α, p-Nitro, Cyclic
Names
[ CAS No. ]:
60477-38-5
[ 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]:
[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]
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