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Nutlin-3 is a small molecule inhibitor of the MDM2/p53 interaction, which leads to the non-genotoxic p53 stabilization, activation of cell cycle arrest and apoptosis pathways. Nutlin-3 inhibits the MDM2-p53 interaction with IC50 of 0.09 μM and synergistically activates p53 to suppress tumor growth. Nutlin-3 induces apoptosis in cancer cells. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM in cells with wild-type p53 such as HCT116, RKO and SJSA-1.
Ecotoxicol Environ Saf. 2022 Jun 1;237:113564.
Environmental BPDE induced human trophoblast cell apoptosis by up-regulating lnc-HZ01/p53 positive feedback loop
Nutlin-3 purchased from AbMole
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Source | Johann Wolfgang Goethe-Universität (2017). Figure 42. Nutlin (AbMole Bioscience; Houston, TX, USA) |
| Method | Western Blot | |
| Cell Lines | UKF-NB-3 und UKF-NB-6 Zellen | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Auch hier ist durch die kombinierte Behandlung mit 10 nM YM155 und 1 μM Nutlin-3 eine 15-fache Erhöhung des p21 Proteinlevels in UKF-NB-3 zu beobachten. Ebenfalls erfolgt ein Anstieg der γH2A.X Expression |
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Source | Johann Wolfgang Goethe-Universität (2017). Figure 41. Nutlin (AbMole Bioscience; Houston, TX, USA) |
| Method | Western Blot | |
| Cell Lines | UKF-NB-3 und UKF-NB-6 Zellen | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Anhand der Quantifizierung ist in Abb. 41 A zu erkennen, dass die Nutlin-3 Behandlung (1 μM) einen signifikanten Anstieg von p53 in UKF-NB-3 bewirkt (3-fach). |
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Source | Johann Wolfgang Goethe-Universität (2017). Figure 40. Nutlin (AbMole Bioscience; Houston, TX, USA) |
| Method | Western Blot | |
| Cell Lines | UKF-NB-3 und UKF-NB-6 Zellen | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Um diesen Effekt genauer zu untersuchen, wurde im Western-Blot geprüft, inwiefern die kombinierte YM155 und Nutlin-3 Behandlung einen Einfluss auf die Expression entsprechender Proteine in UKF-NB-3 und UKF-NB-6 Zellen ausübt |
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Source | Johann Wolfgang Goethe-Universität (2017). Figure 39. Nutlin (AbMole Bioscience; Houston, TX, USA) |
| Method | Western Blot | |
| Cell Lines | UKF-NB-3 und UKF-NB-6 Zellen | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Eine kombinierte Behandlung der UKF-NB-3 und UKF-NB-6 Zellen mit 0,625 nM YM155 und 1 μM Nutlin-3 zeigt einen signifikant verstärkenden Effekt in beiden Zelllinien |
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Source | Vitrual Biology (2015). Figure 3. Nutlin-3 |
| Method | Test for vitality with resazurin | |
| Cell Lines | NSCLC cells | |
| Concentrations | 30 μM | |
| Incubation Time | 24 h | |
| Results | On Figure 3 we selected several pathways that demonstrated an interesting dynamic in the change of significance (measured as -Log2(p-value)) of the moderately resistant cell lines in comparison with sensitive cell lines in different conditions with increased dosage of treatment by Nutlin-3. |
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Source | Vitrual Biology (2015). Figure 1. Nutlin-3 |
| Method | Test of sensitivity of NSCLC cells to Nutlin-3 | |
| Cell Lines | NSCLC cells | |
| Concentrations | 30 μM | |
| Incubation Time | 24 h | |
| Results | For further analysis we selected three cell lines: one, which was the most sensitive to Nutlin-3 – the H1944 cell line, and two, which were still reacting to Nutlin-3, but only under relatively high concentrations – H292 and A427 |
| Cell Experiment | |
|---|---|
| Cell lines | wild-type p53 (HCT116, RKO, and SJSA-1) and mutant p53 (MDA-MB-435 and SW480) cell lines |
| Preparation method | Effect of the enantiomers of Nutlin-3 on the growth and viability of cancer cells with wild-type p53 (HCT116, RKO, and SJSA-1) and mutant p53 (MDA-MB-435 and SW480). Cells were grown, treated, and analyzedAntiproliferative and cytotoxic activity of Nutlin-1. Exponentially growing cancer cells with wild-type p53 (HCT116, RKO, and SJSA-1) or mutant p53 (MDA-MB-435 and SW480) were incubated with a range of concentrations for 5 days and the cell mass and viability were measured by the MTT assay. |
| Concentrations | 0~30µM |
| Incubation time | 5 days |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice bearing subcutaneous human cancer xenografts |
| Formulation | 2% Klucel, 0.5% Tween 80 |
| Dosages | 200 mg/kg twice daily for 3 weeks |
| Administration | oral gavage |
| Molecular Weight | 581.49 |
| Formula | C30H30Cl2N4O4 |
| CAS Number | 548472-68-0 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Secchiero P, et al. Curr Pharm Des. Recent advances in the therapeutic perspectives of Nutlin-3.
| Related Mdm2 Products |
|---|
| NSC 66811
NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. |
| Nutlin-3a
Nutlin-3a, the active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits the p53/MDM2 interaction with IC50 of 90 nM. |
| Nutlin-3b
Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a. |
| SL-01
SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM. |
| NSC 207895
NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
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