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NSC 207895 (XI-006)

MDMX inhibitor,anti-cancer agent CAS# 58131-57-0

NSC 207895 (XI-006)

Catalog No. BCC2243----Order now to get a substantial discount!

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NSC 207895 (XI-006): 5mg $138 In Stock
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Chemical structure

NSC 207895 (XI-006)

3D structure

Chemical Properties of NSC 207895 (XI-006)

Cas No. 58131-57-0 SDF Download SDF
PubChem ID 42640 Appearance Powder
Formula C11H13N5O4 M.Wt 279.25
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 0.4 mg/mL (1.43 mM) in DMSO
Chemical Name 4-(4-methylpiperazin-1-yl)-7-nitro-3-oxido-2,1,3-benzoxadiazol-3-ium
SMILES CN1CCN(CC1)C2=CC=C(C3=NO[N+](=C23)[O-])[N+](=O)[O-]
Standard InChIKey MWFZDJLPWDCQIL-UHFFFAOYSA-N
Standard InChI InChI=1S/C11H13N5O4/c1-13-4-6-14(7-5-13)9-3-2-8(15(17)18)10-11(9)16(19)20-12-10/h2-3H,4-7H2,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of NSC 207895 (XI-006)

DescriptionNSC 207895 is an anticancer agent.
TargetsE3 ligase MDM2MDMX    

NSC 207895 (XI-006) Dilution Calculator

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NSC 207895 (XI-006) Molarity Calculator

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Preparing Stock Solutions of NSC 207895 (XI-006)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.581 mL 17.9051 mL 35.8102 mL 71.6204 mL 89.5255 mL
5 mM 0.7162 mL 3.581 mL 7.162 mL 14.3241 mL 17.9051 mL
10 mM 0.3581 mL 1.7905 mL 3.581 mL 7.162 mL 8.9526 mL
50 mM 0.0716 mL 0.3581 mL 0.7162 mL 1.4324 mL 1.7905 mL
100 mM 0.0358 mL 0.1791 mL 0.3581 mL 0.7162 mL 0.8953 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on NSC 207895 (XI-006)

NSC 207895 is a small-molecule inhibitor of MDMX with GI50 value of 117nM [1].

NSC 207895 is a benzofuroxan derivative and is less toxic. NSC 207895 decreases the activity of MDMX promoter and subsequently decreases both the mRNA and protein levels of MDMX in MCF-7 cells. This inhibition of MDMX is accompanied with the activation of p53. NSC 207895 induces apoptosis in MCF-7 cells since it induces pro-apoptotic gene expression. It is found that the cleavage of PARP is significantly induced by NSC 207895 [2].

NSC 207895 is also found to be a DNA-damaging agent. It shows strong functional interactions with both DNA repair and replication fork complexes. NSC 207895 activates the DNA damage response (DDR) and leads a delay in cell cycle progression [3].

References:
[1] Hawes JJ, Nerva JD, Reilly KM. Novel dual-reporter preclinical screen for antiastrocytoma agents identifies cytostatic and cytotoxic compounds. J Biomol Screen. 2008 Sep;13(8):795-803.
[2] Wang H, Ma X, Ren S, Buolamwini JK, Yan C. A small-molecule inhibitor of MDMX activates p53 and induces apoptosis. Mol Cancer Ther. 2011 Jan;10(1):69-79.
[3] Kapitzky L, Beltrao P, Berens TJ, Gassner N, Zhou C, Wüster A, Wu J, Babu MM, Elledge SJ, Toczyski D, Lokey RS, Krogan NJ. Cross-species chemogenomic profiling reveals evolutionarily conserved drug mode of action. Mol Syst Biol. 2010 Dec 21;6:451.

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Description

NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

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