444158
MDMX Inhibitor, NSC207895
The MDMX Inhibitor, NSC207895 controls the biological activity of MDMX. This small molecule/inhibitor is primarily used for Cancer applications.
别名:
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
产品名称
MDMX Inhibitor, NSC207895, The MDMX Inhibitor, NSC207895 controls the biological activity of MDMX. This small molecule/inhibitor is primarily used for Cancer applications.
SMILES string
CN(CC1)CCN1C(C2=[N]([O-])ON=C23)=CC=C3[N+]([O-])=O
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
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
Other Notes
Wang, H., et al. 2011. Mol. Cancer Ther.7, 611.
Berkson, R.G., et al. 2005. Int. J. Cancer115, 701.
Berkson, R.G., et al. 2005. Int. J. Cancer115, 701.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
General description
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.
存储类别
10-13 - German Storage Class 10 to 13
法规信息
监管及禁止进口产品
此项目有
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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