60477-38-5

60477-38-5 structure

Name: Pifithrin-α, p-Nitro, Cyclic
Chemical Name: 2-(4-Nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
CAS Number: 60477-38-5
Molecular Formula: C₁₅H₁₃N₃O₂S
Molecular Weight: 299.348
Catalog: Signaling Pathways Apoptosis MDM-2/p53
Create Date: 2018-07-05 16:25:51
Modify Date: 2024-01-20 09:56:07
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].

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

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.