SJ-172550

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

第一个小分子 MDMX 抑制剂，可逆地结合 MDMX 的 p53 结合袋。

The first small molecule MDMX inhibitor that reversibly binds the p53-binding pocket of MDMX, disrupts MDMX-p53 interaction with EC50 of 2.3 uM.

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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SJ172550 | SJ 172550

Apoptosis

MDM2-p53

MDM2-p53

Cancer

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431979-47-4

428.8655

C22H21ClN2O5

>98% (HPLC)

10 mM in DMSO

ClC1=CC(/C=C2C(N(C3=CC=CC=C3)N=C\2C)=O)=CC(OCC)=C1OCC(OC)=O

Acetic acid, 2-[2-chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]-, methyl ester

(-20℃)

With Ice Pack

≥ 2 years