PRIMA-1MET (CAS 5291-32-7)
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PRIMA-1MET is a methylated derivative of PRIMA-1 (sc-200927). This compound may act 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.
PRIMA-1,[object Object], (CAS 5291-32-7) References
- PRIMA-1(MET) synergizes with cisplatin to induce tumor cell apoptosis. | Bykov, VJ., et al. 2005. Oncogene. 24: 3484-91. PMID: 15735745
- PRIMA-1MET induces mitochondrial apoptosis through activation of caspase-2. | Shen, J., et al. 2008. Oncogene. 27: 6571-80. PMID: 18663359
- PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein. | Stuber, G., et al. 2009. Mol Cancer. 8: 23. PMID: 19323829
- PRIMA‑1met induces autophagy in colorectal cancer cells through upregulation of the mTOR/AMPK‑ULK1‑Vps34 signaling cascade. | Li, XL., et al. 2021. Oncol Rep. 45: PMID: 33846805
- Ascorbate Inhibits Proliferation and Promotes Myeloid Differentiation in TP53-Mutant Leukemia. | Smith-Díaz, CC., et al. 2021. Front Oncol. 11: 709543. PMID: 34497762
- Transcriptional Regulation of Amino Acid Transport in Glioblastoma Multiforme. | Umans, RA., et al. 2021. Cancers (Basel). 13: PMID: 34944790
- Estrogen Receptor-Beta2 (ERβ2)-Mutant p53-FOXM1 Axis: A Novel Driver of Proliferation, Chemoresistance, and Disease Progression in High Grade Serous Ovarian Cancer (HGSOC). | Oturkar, CC., et al. 2022. Cancers (Basel). 14: PMID: 35267428
- Corrigendum to 'p53 Reactivation by PRIMA-1Met (APR-246) sensitises V600E/KBRAF melanoma to vemurafenib'[Eur J of Cancer 55 (2016) 98-110]. | Krayem, M., et al. 2022. Eur J Cancer. 175: 336-338. PMID: 36167622
- Anti-inflammatory effects of PRIMA-1MET (mutant p53 reactivator) induced by inhibition of nuclear factor-κB on rheumatoid arthritis fibroblast-like synoviocytes. | Adib, M., et al. 2023. Inflammopharmacology. 31: 385-394. PMID: 36350424
- Corrigendum: Current insights into the regulation of programmed cell death by TP53 mutation in cancer. | Su, Y., et al. 2022. Front Oncol. 12: 1071831. PMID: 36439483
- Drugs Targeting p53 Mutations with FDA Approval and in Clinical Trials. | Nishikawa, S. and Iwakuma, T. 2023. Cancers (Basel). 15: PMID: 36672377
- Innovative Therapeutic Approaches for the Treatment of the Ocular Morbidities in Patients with EEC Syndrome. | Barbaro, V., et al. 2023. Cells. 12: PMID: 36766837
- Dexamethasone Selectively Inhibits Detachment of Metastatic Thyroid Cancer Cells during Random Positioning. | Melnik, D., et al. 2023. Cancers (Basel). 15: PMID: 36980530
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PRIMA-1MET, 10 mg | sc-361295 | 10 mg | $153.00 | |||
PRIMA-1MET, 25 mg | sc-361295A | 25 mg | $325.00 |