Pifithrin-α (PFT-α; Item No. 13326) is an inactivator of p53 that blocks p53-dependent transcriptional activation and apoptosis.{17259} Cyclic PFT-α (Item No. 14748) is a stable analog of PFT-α.{23585} p-nitro-Cyclic PFT-α is a cell-permeable form of cyclic PFT-α.{23578} It is one order of magnitude more active that PFT-α in protecting cortical neurons exposed to etoposide (ED50 = 30 nM).{23578} p-nitro-Cyclic PFT-α acts in a p53-dependent manner but does not block phosphorylation of p53 on Ser15 in response to etoposide treatment, although it prevents p53 posttranscriptional activity.{23578} Although it is more stable in solution than the parent compound, this derivative is not active in vivo.{23578}
产品描述
A cell-permeable form of cyclic PFT-α; 10-fold more active that PFT-α in protecting cortical neurons exposed to etoposide (ED50 = 30 nM); not active in vivo
