- Cat. No.
- A10657
Nutlin-3
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.
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MDM2 inhibitors disrupt the binding of mouse double minute 2 homolog (MDM2) to the tumor suppressor p53. In 1992 the MDM2 protein was shown to form a complex with p53 and inhibit p53-mediated transactivation. MDM2 is also an E3 ubiquitin ligase that promotes the rapid degradation of p53, as reported in 1997. Nutlins, reported in 2004, occupy the p53-binding pocket of MDM2 and activate the p53 pathway in cells and in vivo. Nutlin 3a is the active enantiomer of nutlin-3, and Nutlin 3b is a much weaker enantiomer used as a control. RG7112 and APG-115 are further MDM2 inhibitors, while MD-224 is a degrader that removes MDM2 protein. SJ 172550 targets the MDM2 relative MDM4 (also called MDMX).
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.
Synonyms: (+)-Nutlin-3
Nutlin 3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 uM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
Synonyms: SAR405838
MI-773 is an orally available MDM2 antagonist with Ki of 0.88 nM.
Synonyms: (Rac)-Rebemadlin
(Rac)-Nutlin-3 is a potent antagonist of the murine double minute protein 2 (MDM2), with an IC50 of 90 nM. This compound effectively disrupts the interaction between MDM2 and p53, leading to stabilization of the p53 protein. Additionally, (Rac)-Nutlin-3 promotes cell autophagy and apoptosis, making it a valuable tool for investigating the roles of MDM2 in TP53 wild-type ovarian carcinomas and other related cancer research applications.
MI-219 is an MDM2 antagonist with a Ki of 13.3 μM, specifically designed to disrupt the interaction between MDM2 and p53. This compound effectively inhibits the proliferation of FSCCL cells, demonstrated by an IC50 of 2.5 μM. MI-219 is suitable for research applications focused on cancer biology, particularly in studies exploring pathways related to tumor suppression and the p53 signaling axis.
Nutlin 1 is a potent MDM2 antagonist that reactivates the p53 pathway, playing a critical role in cell cycle regulation and apoptosis. With an IC50 of 0.26 μM, it effectively disrupts the MDM2-p53 interaction, promoting p53-mediated transcriptional activity. This compound is widely used in cancer research to explore the therapeutic potential of p53 reactivation in tumor cells.