p-nitro-Pifithrin-α

Pifithrin-α (Item No. 13326) is an inactivator of p53 that blocks p53-dependent transcriptional activation and apoptosis.¹ p-nitro-Pifithrin-α is a cell-permeable analog of pifithrin-α.² It blocks p53-mediated expression of p21/WAF1 and apoptosis in cortical neurons ten-fold more potently than pifithrin-α.² p-nitro-Pifithrin-α, at 10 µM, suppresses p53-mediated TGF-β1 expression in human proximal tubular cells and attenuates steatosis and liver injury in mice fed a high-fat diet.^3,4 It is slowly converted into a more potent cyclized form, p-nitro cyclic pifithrin-α, when incubated in biological media (t_½ = 8 h).²

WARNING This product is not for human or veterinary use.

1. Komarov, P.G., Komarova, E.A., Kondratov, R.V., et al. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285(5434), 1733-1737 (1999).

2. Pietrancosta, N., Moumen, A., Dono, R., et al. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: Discovery of a highly potent in vivo inhibitor and its action mechanism. J. Med. Chem. 49(12), 3645-3652 (2006).

3. Shimizu, H., Yisireyili, M., Nishijima, F., et al. Indoxyl sulfate enhances p53-TGF-β1-Smad3 pathway in proximal tubular cells. Am. J. Nephrol. 37(2), 97-103 (2013).

4. Derdak, Z., Villegas, K.A., Harb, R., et al. Inhibition of p53 attenuates steatosis and liver injury in a mouse model of non-alcoholic fatty liver disease. J. Hepatol. 58(4), 785-791 (2013).

Tufail, Y.Z., Guijas, C., Kummer, D.A., et al. Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism. Cell Chem. Bio. 33(1), 74-90.e19 (2025).