Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nutlin-3 is an MDM2 antagonist.Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; induces apoptosis in Y cells.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 54.00 | |
5 mg | In stock | $ 81.00 | |
10 mg | In stock | $ 126.00 | |
25 mg | In stock | $ 261.00 | |
50 mg | In stock | $ 481.00 | |
100 mg | In stock | $ 522.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 111.00 |
Description | Nutlin-3 is an MDM2 antagonist.Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; induces apoptosis in Y cells. |
Targets&IC50 | MDM2-p53:0.09 μM |
In vitro | Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1 μM of Inauhzin and 2 μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis[2]. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. Nutlin-3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) as a single agent, but has minimal toxicity toward p53-deficient cells (IC50, >10 μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10 μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines[3]. |
In vivo | Nutlin-3 is able to suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model[2]. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo[3]. |
Kinase Assay | Biacore study: Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25°C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculated |
Cell Research | Nutlin-3 (NUT) is dissolved with DMSO (100 mM) and diluted with appropriate media[2]. Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates, and incubated at 37°C overnight. After treatment of Inauhzin and Nutlin-3 at the indicated concentrations for 48 h, cells are harvested, fixed in 70% ice-cold ethanol overnight at -20°C, resuspended in propidium iodide-solution (50 μg/mL PI, 0.1 mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37°C, then analyzed for DNA content using a flow cytometer and proprietary software[2]. |
Synonyms | Nutlin3 |
Molecular Weight | 581.49 |
Formula | C30H30Cl2N4O4 |
CAS No. | 548472-68-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (94.58 mM)
You can also refer to dose conversion for different animals. More
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Nutlin-3 548472-68-0 Ubiquitination E1/E2/E3 Enzyme E3 ligating enzyme E2 conjugating enzyme E1 activating enzyme Ubiquitin conjugating enzyme inhibit MDM-2/p53 Nutlin 3 Ubiquitin activating enzyme Inhibitor Nutlin3 Ubiquitin ligase inhibitor