PRIMA-1MET is a methylated derivative of PRIMA-1 (sc-200927). This compound has been shown to restore mutant p53 activity, and to act synergistically with chemotherapeutic agents to inhibit tumor cell proliferation. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance. Cellular TrxR1 activity is inhibited by PRIMA-1MET irrespective of p53 status. PRIMA-1MET can directly affect cellular redox status via targeting of TrxR1. PRIMA-1MET has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53. PRIMA-1MET treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. PRIMA-1MET is also known as APR-246, 2-(hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one, and 2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one.
1. Bykov, Vladimir J N., et al., 2005. PRIMA-1(MET) synergizes with cisplatin to induce tumor cell apoptosis. Oncogene. 24(21): 3484-91. PMID: 15735745
2. Shen, J., et al., 2008. PRIMA-1MET induces mitochondrial apoptosis through activation of caspase-2. Oncogene. 27(51): 6571-80. PMID: 18663359
3. Stuber, György., et al., 2009. PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein. Molecular cancer. 8(): 23. PMID: 19323829
See how others have used PRIMA-1MET (CAS 5291-32-7). Click on the entry to view the PubMed entry .
PMID: # 30895171 Tessoulin, B.|Descamps, G.|Dousset, C.|Amiot, M.|Pellat-Deceunynck, C.| et al. 2019. Front Oncol. 9: 128.
PMID: # 26986846 Yoshikawa, N. et al. 2016. Oncol. Rep. 35: 2543-52.
PMID: # 27533080 Venkatesan, S. et al. 2016. Oncotarget. 7: 58435-58444.
PMID: # 26463477 Grellety, T.|Laroche-Clary, A.|Chaire, V.|Lagarde, P.|Chibon, F.|Neuville, A.|Italiano, A.| et al. 2015. BMC Cancer. 15: 684.
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 © 2007-2020 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.