Nutlin-3

- Overview
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    Background
    
    Nutlin-3, a tetra-substituted imidazoline, is a potent and selective small-molecule antagonist of murine double minute 2 (MDM2), which occupies the binding site of p53 in MDM2 and consequently prevent MDM2 binding to p53 leading to the disruption of the autoregulator feedback loop and the fostering of the p53 tumor suppressor network. It also binds to murine double minute 4 (MDM4), which is another component of the p35 tumor surveillance pathway. Nutlin-3 is being investigated as an antitumor agent for its antiangiogenic activity in cells through inhibiting endothelial cell migration, inducing cell cycle arrest, and increasing apoptotic tendency in endothelial cells.
- Properties
  - Alternative Name
    
    Nutlin 3,MDM2 Antagonist; 4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
    
    CAS Number
    
    890090-75-2
    
    Molecular Formula
    
    C30H30Cl2N4O4
    
    Molecular Weight
    
    581.5
    
    Appearance
    
    A solid
    
    Purity
    
    96.76%
    
    Solubility
    
    ≥58.2 mg/mL in DMSO; insoluble in H2O; ≥5.69 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Xiyao Cheng, Rong Chen, et al. "Leveraging the multivalent p53 peptide-MdmX interaction to guide the improvement of small molecule inhibitors." Nat Commun. 2022 Feb 28;13(1):1087. PMID:35228542
    2. Priscilla Cheung, Jordi Xiol, et al. "Regenerative Reprogramming of the Intestinal Stem Cell State via Hippo Signaling Suppresses Metastatic Colorectal Cancer." Cell Stem Cell. 2020 Oct 1;27(4):590-604.e9. PMID:32730753

Nutlin-3

Background

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