NUTLIN-3

(±)-Nutlin-3 is a racemic mixture of the p53-Mdm2 protein-protein interaction inhibitor (−)-nutlin-3 and its less active enantiomer (+)-nutlin-3 . In vivo, (±)-nutlin-3 (200 mg/kg twice daily) reduces tumor volume in an SJSA-1 osteosarcoma mouse xenograft model.

(+/-)-Nutlin-3 is a small molecule MDM2 antagonist.

ChEBI: 4-[[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazol-1-yl]-oxomethyl]-2-piperazinone is a stilbenoid.

reagent type: ligand

Nutlin-3, an antagonist of a human homolog of murine double minute 2 (HDM2). It has the ability to inhibit the HDM2-directed degradation of p53. Nutlin-3 can also enhance the transcriptional activities of p73.

Store at -20°C

[1] LYUBOMIR T. VASSILEV. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2[J]. Science, 2004, 303 5659. DOI:10.1126/science.1092472
[2] SARA GHASSEMIFAR  Susan M M. MDM2 antagonism by nutlin-3 induces death in human medulloblastoma cells[J]. Neuroscience Letters, 2012, 513 1: Pages 106-110. DOI:10.1016/j.neulet.2012.02.022
[3] VALENTINA MANFÉ . MDM2 Inhibitor Nutlin-3a Induces Apoptosis and Senescence in Cutaneous T-Cell Lymphoma: Role of p53[J]. Journal of Investigative Dermatology, 2012, 132 5: Pages 1487-1496. DOI:10.1038/jid.2012.10
[4] ANNETTE KÜNKELE. Pharmacological activation of the p53 pathway by nutlin-3 exerts anti-tumoral effects in medulloblastomas.[J]. Neuro-oncology, 2012, 14 7: 859-869. DOI:10.1093/neuonc/nos115