Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. It enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin (sc-280681), etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation, and does not induce visible tumors. Protects against neuronal death in models of stroke and neurodegenerative disorders. Pifithrin-α is also an aryl hydrocarbon receptor (AHR) agonist, which leads to the upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
1. Komarov, P G., et al., 1999. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science (New York, N.Y.). 285(5434): 1733-7. PMID: 10481009
2. Komarova, E A., et al., 2000. Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry. Biokhimia. 65(1): 41-8. PMID: 10702639
3. Culmsee, C., et al., 2001. A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid beta-peptide. Journal of neurochemistry. 77(1): 220-8. PMID: 11279278
4. Lorenzo, Elisa., et al., 2002. Doxorubicin induces apoptosis and CD95 gene expression in human primary endothelial cells through a p53-dependent mechanism. The Journal of biological chemistry. 277(13): 10883-92. PMID: 11779855
5. Hoagland, Martin S., et al., 2005. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor. The Journal of pharmacology and experimental therapeutics. 314(2): 603-10. PMID: 15843497
6. Sohn, D., et al., 2009. Pifithrin-alpha protects against DNA damage-induced apoptosis downstream of mitochondria independent of p53. Cell death and differentiation. 16(6): 869-78. PMID: 19229248
See how others have used Pifithrin-alpha hydrobromide. Click on the entry to view the PubMed entry .
PMID: # 28608259 Qiu, M. et al. 2017. Cancer Chemother. Pharmacol. 80: 275-286.
PMID: # 27464000 Zhang, Y. et al. 2016. Autophagy. 12: 1538-59.
PMID: # 26884717 Yu, W. et al. 2016. Int. J. Biol. Sci. 12: 198-209.
PMID: # 26431790 Yin, R. et al. 2016. Respir Physiol Neurobiol. 220: 81-7.
PMID: # 25466893 Liu, W. et al. 2015. FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 29: 1113-23.
PMID: # 25727698 Wang, Y. et al. 2015. J. Neurochem. 133: 828-43.
PMID: # 24722580 Moretti, RM. et al. 2014. PloS one. 9: e93713.
PMID: # 25193078 Das, A. et al. 2014. Exp. Cell Res. 328: 361-78.
PMID: # 24946002 Sun, H. et al. 2014. Br. J. Cancer. 111: 281-91.
PMID: # 21521785 Verma, S. et al. 2011. Blood. 117: 6600-7.
Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.