NSC 207895 (XI-006)

An inhibitor of MDMX

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库存: 现货

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5mg

￥1050.00

840.00

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10mg

￥2100.00

1680.00

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50mg

￥5887.00

4710.00

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200mg

￥12975.00

10380.00

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货号: ajci9644
CAS: 58131-57-0
别名: 4-(4-甲基-1-哌嗪基)-7-硝基-2,1,3-苯并二唑3-氧化物,XI-006
分子式: C11H13N5O4
分子量: 279.25
纯度: >98%
溶解度: DMF: 15 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2mg/mL,DMSO: 2 mg/mL,Ethanol: 1 mg/mL
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.