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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-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas. Nutlin-3a effectively arrestes cell-cycle progression in all cell lines, depleting the S-phase compartment to 0.2-2% and increasing the G1- and G2/M-phase compartments, indicating G1 and G2 arrest.
Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200 mg/kg) showing a substantial tumor shrinkage (eight partial and one full regressions). The established SJSA-1 and MHM osteosarcoma xenografts with Nutlin-3a causes extensive tumor regression.
Neural Regen Res. 2024 Jul 11;119:111165.
Impacts of Nutlin-3a and exercise on murine double minute 2–enriched glioma treatment
Nutlin-3a purchased from AbMole
| Molecular Weight | 581.49 |
| Formula | C30H30Cl2N4O4 |
| CAS Number | 675576-98-4 |
| Solubility (25°C) | DMSO 85 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Jill E Kucab, et al. Nutlin-3a selects for cells harbouring TP53 mutations
| Related Mdm2 Products |
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| Nutlin-3
Nutlin-3 is a selective MDM2 (mouse double minute 2) antagonist with IC50 of 90 nM. 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. |
| 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-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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