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Nutlin-3
- Soluble in DMSO and EtOH
- MF: C30H30Cl2N4O4
- MW: 581.49
Description
Nutlin-3 is an MDM2 antagonist that binds the p53-binding pocket of MDM2 and stabilizes p53 in cells with functional p53 signaling.
Disrupting the MDM2-p53 interaction activates p53-dependent transcription, cell-cycle arrest and apoptosis. Nutlin-3 is a benchmark tool for studying p53 reactivation, tumor suppressor signaling and MDM2 inhibitor pharmacology.
Key Features
- MDM2 antagonist targeting the p53-binding pocket
- Stabilizes and activates p53 signaling
- Induces p53-dependent cell-cycle arrest and apoptosis
- Reference tool for MDM2-p53 pathway research
Applications
- p53 pathway activation studies
- MDM2 inhibitor pharmacology
- Cancer cell apoptosis assays
- Tumor suppressor signaling research
Related compounds: Its two enantiomers, the more active (-)-enantiomer Nutlin-3a (Axon 1880) and the less active (+)-enantiomer Nutlin-3b (Axon 1881), are also available.
More Information
| Parent CAS No. | 548472-68-0 |
|---|---|
| Chemical Name | 4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one |
| MFCD | MFCD07784509 |
| Short Description | MDM2 inhibitor |
References
- LT Vassilev et al. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2. Science 2004, 303, 844-848.
- S Shangary and S Wang. Small-Molecule Inhibitors of the MDM2-p53 Protein-Protein Interaction to Reactivate p53 Function: A Novel Approach for Cancer Therapy. Ann. Rev. Pharmacol. Toxicol. 2008, 49: 223–241.
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