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444152 Sigma-Aldrich

MDM2 Antagonist IV, Nutlin-3a - CAS 675576-98-4 - Calbiochem

The MDM2 Antagonist IV, Nutlin-3a, also referenced under CAS 675576-98-4, controls the biological activity of MDM2. This small molecule/inhibitor is primarily used for Cancer applications.

Synonym: (-)-4-(4,5- bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one, (-)-4-(4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one, MDM2 Antagonist IV, Nutlin-3a - CAS 675576-98-4 - Calbiochem

  • CAS Number 675576-98-4

  • Empirical Formula (Hill Notation) C30H30Cl2N4O4

  • Molecular Weight 581.49

  •  MDL number MFCD14636430

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Properties

Quality Level   100
assay   ≥98% (HPLC)
form   powder
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   white
solubility   DMSO: 100 mg/mL
shipped in   ambient

Description

General description

A cell-permeable and highly potent active enantiomer of Nutlin-3 (Cat. No. 444143) that binds to the p53-binding pocket and blocks the interaction of p53 and MDM2 (IC50 = 90 nM). Exhibits over 150-fold greater affinity for MDM2 than its less active enantiomer, Nutlin-3b. Induces p53 mediated apoptosis by both transcription-dependent and independent mechanisms. Shown to greatly potentiate the cytotoxic effects of chemotherapeutic agents and reduce tumor burden in vivo. Also shown to overcome ATM-mediated resistance to fludarabine in chronic lymphocyte leukemia. Cells treated with Nutlin-3a permanently lose their ability to proliferate and enter into a pattern of permanent senescence. Mouse embryonic fibroblasts with p53+/+MEFs show significantly reduced reprogramming capabilities following Nutlin-3a treatment.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ohnstad, H.O., et al. 2011. BMC Cancer11, 211.
Shen, H. and Maki, C.G., 2010. J. Biol. Chem.285, 23105.
Kawamura, T., et al. 2009. Nature460, 1140.
Kojima, K., et al. 2006. Blood108, 993.
Laurie, N.A., et al. 2006. Nature444, 61.
Tovar, C., et al. 2006. Proc. Natl. Acad. Sci. USA103, 1888.
Vassilev, L.T. 2006. Trends Mol Med.13, 23.
Thompson, T., et al. 2004. J. Biol. Chem.279, 53015.
Vassilev, L.T., et al. 2004. Science303, 844.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
Peer-Reviewed Papers
15

References

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