SJ 172550

A small molecule inhibitor of MDMX

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10mg

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50mg

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货号: ajci11422
CAS: 431979-47-4
别名: MDMX Inhibitor II
分子式: C22H21ClN2O5
分子量: 428.87
纯度: >98%
溶解度: DMF: 30 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: slightly
储存: Store at 4°C
库存: 现货

Background

SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.

The p53 pathway is disrupted in virtually every human tumor. SJ-172550 binds the p53-binding pocket of MDMX, thereby displacing p53. SJ-172550 binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified. The effect of SJ-172550 is additive when combined with an MDM2 inhibitor nutlin-3a[1]. SJ-172550 acts through a complicated mechanism in which the compound forms a covalent but reversible complex with MDMX and locks MDMX into a conformation that is unable to bind p53. The relative stability of this complex is influenced by many factors including the reducing potential of the media, the presence of aggregates[2].

参考文献:
[1]. Reed D, et al. Identification and characterization of the first small molecule inhibitor of MDMX. J Biol Chem. 2010 Apr 2;285(14):10786-96.
[2]. Bista M, et al. On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. PLoS One. 2012;7(6):e37518.