Cyclic Pifithrin-α hydrobromide is a cyclic analog of pifithrin-α a small molecule inhibitor of p53. It reversibly inhibits p53-dependent transactivation of p53-responsive genes and reversibly blocks p53-mediated apoptosis, with less cytotoxicity than the parent compound. Potent STAT6 transcriptional inhibitor. This compound has been shown to prevent dexamethasone-induced cell death in murine thymocytes with an EC50value of 2.01 µM. Sensitizes p53-deficient tumors to radiotherapy and chemotherapy; increases apoptosis in target cells when used in combination with antimicrotubule agents.
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PMID: # 25746954 Lima, CF. et al. 2015. Eur J Pharm Sci. 72: 34-45.
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