NUTLIN-3

Description

(±)-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.

The Uses of NUTLIN-3

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

What are the applications of Application

Nutlin-3 is an apoptosis inducer and disruptor of MDM2-p53 interaction, inhibiting with a IC50 of 0.09 μM.

Definition

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.

Biochem/physiol Actions

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.

storage

Store at -20°C

References

1) Vassilev et al. (2004), In vivo activation of the p53 pathway by small-molecule antagonists of MDM2; Science, 303 844 2) Ghassemifar et al. (2012), MDM2 antagonism by nutlin-3 induces death in human medulloblastoma cells; Neurosci. Lett., 513 106 3) Manfe et al. (2012), MDM2 inhibitor nutlin-3 induces apoptosis and senescence in cutaneous T-cell lymphoma: role of p53; J. Invest. Dermatol., 132 1487 4) Kunkele et al. (2012), Pharmacological activation of the p53 pathway by nutlin-3 exerts anti-tumoral effects in medulloblastomas; Neuro. Oncol., 14 859