NSC 207895

Name: NSC 207895
Brand: Selleck Chemicals
SKU: S2678
Rating: 5 (5 reviews)

For research use only.

Catalog No.S2678 Synonyms: XI-006

5 publications

CAS No. 58131-57-0

NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

Selleck's NSC 207895 has been cited by 5 publications

Genes Dev, 2020, 34(7-8):526-543

PubMed: 32079652 ( click the link to review the publication )

Oncotarget, 2020, 11(46):4224-4242

PubMed: 33245718 ( click the link to review the publication )

Sci Rep, 2019, 9(1):1897

PubMed: 30760778 ( click the link to review the publication )

Oncol Lett, 2018, 15(2):1673-1679

PubMed: 29434862 ( click the link to review the publication )

Stem Cell Reports, 2016, 7(6):1140-1151

PubMed: 27916539 ( click the link to review the publication )

1 Customer Review

Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).

Stem Cell Reports, 2016, 7:1140-1151.. NSC 207895 purchased from Selleck.

Purity & Quality Control

Choose Selective Mdm2 Inhibitors

Biological Activity

Description

NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

Targets

p53 ^[1]	MDMX ^[1]
	2.5 μM

In vitro

NSC-207895 decreases both the MDMX mRNA and protein in MCF-7 cells. NSC-207895 induces expression of p53 as well as well-characterized p53-target gene, p21 and MDM2, in a dose-dependent manner in MCF-7 cells. NSC-207895 extends the half-life of p53 from 20 to 30 minutes to more than 3 hours as revealed by cycloheximide chase assays in MCF-7 cells. NSC-207895 also activates p53 and induces p21 and MDM2 expression in LNCaP prostate and A549 lung cancer cells. NSC-207895 increases the mRNA levels of proapoptotic genes including PUMA, BAX, and PIG3 in a dose-dependent manner in MCF-7 cells. NSC-207895 results in a significant increase in the numbers of sub-G0/G1 cells as well as G2 arrest. NSC-207895 also results in more than 40% of cells dying via apoptosis and decreases cell viability in A549 and LNCaP cells. ^[1] NSC-207895 inhibits biosynthesis of nucleic acids and proteins in L1210 cells. ^[2] NSC-207895 interacts with DNA repair to activate the DNA damage repair pathway in three species (S. cerevisiae, S. pombe and H. sapiens). ^[3] NSC-207895 acts as cytotoxic agent in the G/R-luc astrocytoma cell line with GI50 of 117 nM. ^[4]

Protocol

Cell Research:

^[1]

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Cell lines: MCF-7 cell
Concentrations: 1-10 μM
Incubation Time: 2 days
Method:
MCF-7 cells treated with dimethyl sulfoxide (DMSO), nutlin-3a, or NSC-207895 are permeabilized with cold 70% ethanol overnight, and stained with a solution containing 50 μg/mL propidium iodide and 20 μg/mL RNase A at 37°C for 20 minutes. The cells are then subjected to flow cytometry analysis. The FlowJo software is used to calculate percentages of cells in each cell cycle phase. For terminal deoxynucleotidyl transferase–mediated dUTP nick end labeling (TUNEL) staining, MCF-7 cells treated with the NSC-207895 for 2 days are fixed with 4% paraformadelhyde for 1 hour, and then subjected to dUTP labeling using In Situ Cell Death Detection Kit TMR Red according to the manufacturer's protocol. For quantitation, at least 300 cells are randomly chosen and the numbers of TUNEL-positive cells are counted.

(Only for Reference)

References

[4] Hawes JJ, et al. J Biomol Screen, 2008, 13(8), 795-803.

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Solubility (25°C)

In vitro	DMSO	0.4 mg/mL (1.43 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download NSC 207895 SDF

Molecular Weight	279.25
Formula	C₁₁H₁₃N₅O₄
CAS No.	58131-57-0
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	XI-006
Smiles	CN1CCN(CC1)C2=CC=C(C3=NO[N+](=C23)[O-])[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

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Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Mdm2 Signaling Pathway Map

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Nutlin-3

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.
Nutlin-3a

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

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Nutlin-3b

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NSC 207895