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SJ-172550

CAS No. : 431979-47-4

MCE 国际站：SJ-172550

产品活性：SJ-172550是MDMX的小分子抑制剂; 与野生型p53肽竞争性结合于MDMX的EC₅₀值为5 μM。

研究领域：Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：MDM-2/p53  |  E1/E2/E3 Enzyme

In Vitro: 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. 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.

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