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NSC 66811 is a potent MDM2 inhibitor with Ki value of 120 nM, which disrupts MDM2-p53 interaction and activates p53 function. NSC-66811 induces p21, p53 and MDM2 accumulation in human colon cancer cells in vitro. NSC 66811 is more potent than the natural p53 peptide to bind with MDM2.
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Source | Acta Pharmacol Sin (2015). Figure 2. NSC 66811 |
| Method | PCR | |
| Cell Lines | HepG2 cells | |
| Concentrations | 5 and 25 μmol/L | |
| Incubation Time | 24 h | |
| Results | The p53 mRNA levels were up-regulated by NSC 66811 (Figure 2F) without affecting the CYP expression. NSC 66811 decreased the metabolism of DEM (Figure 2G) and TEST (Figure 2H) in a dose-dependent manner. |
| Molecular Weight | 340.42 |
| Formula | C23H20N2O |
| CAS Number | 6964-62-1 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mdm2 Products |
|---|
| 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. |
| 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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