pifithrin

Pifithrin is a small molecule inhibitor of the tumor suppressor protein p53 (TP53). It was originally identified for its ability to protect cells from p53-mediated apoptosis induced by DNA-damaging agents or radiation. Pifithrin-alpha, the most common analog, acts by reversibly inhibiting p53-dependent transcriptional activity and mitochondrial translocation. While widely used as a research tool to investigate p53 signaling pathways in various models, including cancer and neuroprotection, it has not reached clinical approval. In the context of oncology research, it is often used to validate the role of p53 in suppressing endogenous retroviruses or to model p53-deficient states in cell lines.

Other names

pifithrin-alpha2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone