Pifithrin-α, p-Nitro, Cyclic

60477-38-5

299.35

10 mM in DMSO

Apoptosis

Pifithrin-alpha, p-Nitro, Cyclic (PFN-alpha) is cell-permeable and active-form p53 inhibitor. Pifithrin-alpha, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-alpha in protecting cortical neurons exposed to Etoposide (ED₅₀=30 nM). Pifithrin-alpha, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-alpha, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue^[1][2]. In Vitro: Pifithrin-alpha, p-Nitro, Cyclic (PFN-alpha) 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-alpha^[1]. In Vivo: Intraocular injection of pifithrin-alpha slightly increases survival of retinal ganglion cell (RGC) at the concentration of 6 uM but not at 0.06 uM. Pifithrin-alpha, p-Nitro, Cyclic (PFN-alpha) is not effective in vivo, even at 6 uM^[1].
Pifithrin-alpha, p-Nitro, Cyclic shows the half-life (t_1/2) of 6 hours (when incubated in biological conditions)^[1].