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Cat. No. Name Size Price Add Cart
KI3470NSC-207895 (XI-006)QuoteQuote

Chemical Characteristic

Product NameNSC-207895 (XI-006)
CAS No.58131-57-0
Molecular Weight 279.25
FormulaC11H13N5O4
Chemical Name2,1,3-Benzoxadiazole, 4-(4-methyl-1-piperazinyl)-7-nitro-, 3-oxide
Smilesn1on(c2c(ccc(c12)[N](=O)O)N1CCN(CC1)C)O
Chemical Structure

Biological activities

NSC-207895 is a MDM2-related protein suppressor that leads to activation of p53. NSC-207895 decreases both the MDMX mRNA and protein levels in MCF-7 cells in vitro.[1] NSC-207895 induces expression of p53 as well as p53-target gene, p21 and MDM2 in MCF-7 cells in a dose-dependent manner. In another in vitro test, NSC-207895 causes a significant increase in the numbers of sub-G0/G1 cells as well as G2 arrest 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 induces apoptosis and inhibits cancer cell growth through inhibition of MDMX expression in MCF-7, A549 and LNCaP cells.[1] NSC-207895 dose-dependently elevates the mRNA levels of proapoptotic genes including PUMA, BAX, and PIG3 in MCF-7 cells. In MCF-7 cells, NSC-207895 cooperates with the MDM2 inhibitor nutlin-3a to activate p53 and decrease cell survival. NSC-207895 results in more than 40% of cells dying via apoptosis with the concentration of 5µM for 5 days in MCF-7 cells. NSC-207895 also induces inhibition of nucleoside uptake and phosphorylation, DNA, RNA, and protein synthesis, as well as degradation of DNA in L1210 cells.[2]

Protocols

NSC-207895 is dissolved in N, N??dimethyformaide in vitro.[2]

References

[1] 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, 10(1):69-79.
[2] Kessel D, Belton JG. Effects of 4-nitrobenzofurazans and their N-oxides on synthesis of protein and nucleic acid by murine leukemia cells. Cancer Res. 1975, 35(12):3735-3740.

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