NSC-207895 | CAS# 58131-57-0 | MDMX inhibitor

MedKoo Cat#: 574087 | Name: NSC-207895

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NSC-207895 is an inhibitor of the p53-binding protein MDMX. NSC 207895 decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21). It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines selectively over wild-type and p53-null osteosarcoma cells

Chemical Structure

NSC-207895

CAS#58131-57-0

Theoretical Analysis

MedKoo Cat#: 574087

Name: NSC-207895

CAS#: 58131-57-0

Chemical Formula: C11H13N5O4

Exact Mass: 279.0968

Molecular Weight: 279.26

Elemental Analysis: C, 47.31; H, 4.69; N, 25.08; O, 22.92

Price and Availability

Size	Price	Availability	Quantity
1mg	USD 255.00
5mg	USD 500.00
10mg	USD 825.00
25mg	USD 1,600.00

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Synonym

NSC-207895, NSC207895, NSC 207895, NSC179940, NSC-179940, NSC 179940, XI-006, XI 006, XI006

IUPAC/Chemical Name

4-(4-methyl-1-piperazinyl)-7-nitro-2,1,3-benzoxadiazole, 3-oxide

InChi Key

MWFZDJLPWDCQIL-UHFFFAOYSA-N

InChi Code

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

SMILES Code

CN1CCN(C2=CC=C([N+]([O-])=O)C3=NO[N+]([O-])=C32)CC1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

NSC-207895 (XI-006), a DNA damaging agent, is an anticancer agent and p53 activator.

In vitro activity:

Then, SA-β-gal staining and P21 (red) staining showed that miR-325-3p decreased mechanical overloading-induced chondrocyte senescence with reduced SA-β-gal positive cells and p21 positive cells, but this effect was attenuated when treating with p53 activator NSC-207895 (Fig. 6E–G). The qRT-PCR and western blot demonstrated that NSC-207895 reduced the effect of miR-325-3p mimic on down-regulating P16, P21, and P53 expression at mRNA and protein levels, respectively (Fig. 6H–J). Meanwhile, miR-325-3p reduced the expression of SASP factors PAI-1, IL-6, and TGF-β; however, NSC-207895 reduced the effect of miR-325-3p to downregulate SASP factors (Fig. 6H). Reference: Arthritis Res Ther. 2023 Apr 4;25(1):54. https://pubmed.ncbi.nlm.nih.gov/37016437/

In vivo activity:

To further validate these in vitro findings, this study tested the effectiveness of MDM4 inhibition in a HepT1 orthotopic xenograft mouse model. Intrahepatic tumors were generated using HepT1 cells transduced with luciferase to allow bioluminescence imaging (BLI) and treated with either NSC207895 or placebo. The HepT1-derived tumors treated with NSC207895 were significantly smaller than the tumors treated with vehicle (NSC207895-treated tumors were 58.01% the weight of placebo-treated tumors, p = 0.0079) (Fig. 8c). Reference: Sci Rep. 2021 Feb 3;11(1):2967. https://pubmed.ncbi.nlm.nih.gov/33536467/

	Solvent	mg/mL	mM
Solubility
	DMF	15.0	53.71
	DMF:PBS (pH 7.2) (1:4)	0.2	0.72
	DMSO	11.2	40.17
	Ethanol	1.0	3.58

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 279.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhao J, Li C, Qin T, Jin Y, He R, Sun Y, Liu Z, Wu T, Duan C, Cao Y, Hu J. Mechanical overloading-induced miR-325-3p reduction promoted chondrocyte senescence and exacerbated facet joint degeneration. Arthritis Res Ther. 2023 Apr 4;25(1):54. doi: 10.1186/s13075-023-03037-3. PMID: 37016437; PMCID: PMC10071751. 2. Pishas KI, Adwal A, Neuhaus SJ, Clayer MT, Farshid G, Staudacher AH, Callen DF. XI-006 induces potent p53-independent apoptosis in Ewing sarcoma. Sci Rep. 2015 Jun 22;5:11465. doi: 10.1038/srep11465. Erratum in: Sci Rep. 2015;5:13328. PMID: 26095524; PMCID: PMC4476092. 3. Woodfield SE, Shi Y, Patel RH, Chen Z, Shah AP, Srivastava RK, Whitlock RS, Ibarra AM, Larson SR, Sarabia SF, Badachhape A, Starosolski Z, Ghaghada KB, Sumazin P, Annis DA, López-Terrada D, Vasudevan SA. MDM4 inhibition: a novel therapeutic strategy to reactivate p53 in hepatoblastoma. Sci Rep. 2021 Feb 3;11(1):2967. doi: 10.1038/s41598-021-82542-4. Erratum in: Sci Rep. 2021 Oct 1;11(1):19916. PMID: 33536467; PMCID: PMC7859402.

In vitro protocol:

In vivo protocol:

1. Woodfield SE, Shi Y, Patel RH, Chen Z, Shah AP, Srivastava RK, Whitlock RS, Ibarra AM, Larson SR, Sarabia SF, Badachhape A, Starosolski Z, Ghaghada KB, Sumazin P, Annis DA, López-Terrada D, Vasudevan SA. MDM4 inhibition: a novel therapeutic strategy to reactivate p53 in hepatoblastoma. Sci Rep. 2021 Feb 3;11(1):2967. doi: 10.1038/s41598-021-82542-4. Erratum in: Sci Rep. 2021 Oct 1;11(1):19916. PMID: 33536467; PMCID: PMC7859402.

1. Wang, H., Ma, X., Ren, S., et al. A small-molecule inhibitor of MDMX activates p53 and induces apoptosis. Mol. Cancer Ther. 10(1), 69-79 (2011). 2. Pishas, K.I., Adwal, A., Neuhaus, S.J., et al. XI-006 induces potent p53-independent apoptosis in Ewing sarcoma. Sci. Rep. 5:11465, (2015).