Nutlin-3 (890090-75-2) Description:
Nutlin-3, the racemic and most commonly used form of nutlin, inhibits p53-MDM2 interaction. It has shown ability to induce the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53, but not in cells with mutated p53. When in combination with perifosine, anti-leukaemic activity has been observed. High N-MYC (MycN) expression has been induced in non-N-MYC-amplified neuroblastoma cells when treated with the combination of nutlin-3 and doxorubicin (sc-200923).
Nutlin 3 is also a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin 3 (2-10 μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3 μM) 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.
Nutlin-3 (890090-75-2) Specifications:
|Synonym||548472-68-0; 890090-75-2; Nutlin 3|
|Color||White to off-white|
|Solubility||Soluble in DMSO (~20 mg/ml)|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||Inhibits p53-MDM2 interaction|