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444158

Sigma-Aldrich

MDMX Inhibitor, NSC207895

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

Synonym(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

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About This Item

Empirical Formula (Hill Notation):
C11H13N5O4
CAS Number:
58131-57-0
Molecular Weight:
279.25
UNSPSC Code:
12352200

Quality Level

100

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

dark red

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

CN(CC1)CCN1C(C2=[N]([O-])ON=C23)=CC=C3[N+]([O-])=O

General description

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.

Packaging

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

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

Legal Information

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

Storage Class Code

10-13 - German Storage Class 10 to 13

Regulatory Information

监管及禁止进口产品

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Rachel G Berkson et al.
International journal of cancer, 115(5), 701-710 (2005-02-25)
Activation of the p53 tumour suppressor is predicted to have therapeutically beneficial effects. Many current anti-cancer therapies activate the p53 response via DNA damage. Non-genotoxic activation of the p53 pathway would open the way to long-term and possibly prophylactic treatments.
Divya Venkatesh et al.
Genes & development, 34(7-8), 526-543 (2020-02-23)
MDM2 and MDMX, negative regulators of the tumor suppressor p53, can work separately and as a heteromeric complex to restrain p53's functions. MDM2 also has pro-oncogenic roles in cells, tissues, and animals that are independent of p53. There is less

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