444158

MDMX Inhibitor, NSC207895

The MDMX Inhibitor, NSC207895 controls the biological activity of MDMX. This small molecule/inhibitor is primarily used for Cancer applications.

• Synonyme(s) : MDMX Inhibitor, NSC207895, 7-(4-Methylpiperazin-1-yl)-4-nitro-2,1,3-benzoxadiazole-1-oxide, 7-(4-Methylpiperazin-1-yl)-4-nitro-1-oxido-2,1,3-benzoxadiazol-1-ium, XI-006
• Formule empirique (notation de Hill): C₁₁H₁₃N₅O₄
• Numéro CAS: 58131-57-0
• Poids moléculaire : 279.25
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: dark red
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: CN(CC1)CCN1C(C2=[N]([O-])ON=C23)=CC=C3[N+]([O-])=O

Description

Description générale

A cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC₅₀ = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation. A great complement to MDM2 antagonist Nutlin-3 (Cat. Nos. 444143 & 444151) in growth inhibition and apoptosis induction of cancer cells that are more sensitive to MDMX than MDM2 inhibition.

A cell-permeable benzofuroxan compound that is shown to downregulate the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC₅₀ = 2.5 µM in HT1080 reporter assays), leading to enhanced p53 stabilization/activation and an upregulation of the p53 downstream gene MDM2 production, which in turn could mediate further cellular MDMX proteolytic degradation. A great complement to MDM2 antagonist Nutlin-3 (Cat. Nos. 444143 & 444151) in growth inhibition of cancer cells that are more sensitive to MDMX than MDM2 inhibition, such as MCF-7 (72% vs. 42% growth inhibition by 5 µM XI-006 and Nutlin-3a, respectively, in 4 days.), where MDMX, but not MDM2, inhibition results in apoptosis induction.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Wang, H., et al. 2011. Mol. Cancer Ther.7, 611.
Berkson, R.G., et al. 2005. Int. J. Cancer115, 701.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 10-13 - German Storage Class 10 to 13