Nutlin-3, the racemic and most commonly used form of nutlin, inhibits p53-MDM2 interaction. It has shown ability to induce the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells. Disrupts MDM2-p53 interaction, inducing apoptosis.
1.Dongjuan Si, Huijuan Luo, Xiaomeng Zhang, Kundi Yang, Hongmei Wen, Wei Li, Jian Liu. (2021) Design, synthesis and biological evaluation of novel pyrrolidone-based derivatives as potent p53-MDM2 inhibitors. BIOORGANIC CHEMISTRY, 115 (105268). [PMID:34426149][10.1016/j.bioorg.2021.105268]
References
1.Ghassemifar S & Mendrysa SM. (2012) MDM2 antagonism by nutlin-3 induces death in human medulloblastoma cells.. Neurosci Lett, 513 (106-10). [PMID:22343310]
2.Sun Z et al.. (2021) Silencing Ribosomal Protein L22 Promotes Proliferation and Migration, and Inhibits Apoptosis of Gastric Cancer Cells by Regulating the Murine Double Minute 2-Protein 53 (MDM2-p53) Signaling Pathway.. Med Sci Monit, 27 (e928375). [PMID:34050122]
3.Shangary S & Wang S. (2009) Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy.. Annu Rev Pharmacol Toxicol, 49 (223-41). [PMID:18834305]
4.Dongjuan Si, Huijuan Luo, Xiaomeng Zhang, Kundi Yang, Hongmei Wen, Wei Li, Jian Liu. (2021) Design, synthesis and biological evaluation of novel pyrrolidone-based derivatives as potent p53-MDM2 inhibitors. BIOORGANIC CHEMISTRY, 115 (105268). [PMID:34426149][10.1016/j.bioorg.2021.105268]
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