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|444153-10MG||Glass bottle||10 mg||
|Overview||A cell-permeable indolyl-hydantoin compound that simultaneously inhibits the interaction of both, MDM2 and MDMX with p53 (IC50 = 17.3 and 24.7 nM, respectively, in vitro). Releases p53 from MDMX inhibition, stabilizes it, and fully restores its function. Shown to be far more superior to Nutlin-3a (Cat. No. 444152) in blocking p53 interaction with MDMX. Binds to Phe, Trp, and Leu sub-pockets on the surface of MDMX and MDM2, and promotes MDMX and MDM2 dimer formation. Shown to induce cell cycle arrest in G1 and G2 phases. Also reported to induce apoptosis in several tumor cell lines expressing wild-type p53/MDMX (~ 10 to 20 µM). Its actions are not believed to be due to any genotoxic stress.|
|Synonyms||MDM2 Inhibitor VIII, MDMX Inhibitor III, (Z)-2-(4-((6-Chloro-7-methyl-1H-indol-3-yl)methylene)-2,5-dioxoimidazolidin-1-yl)-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide, MDM2 Antagonist V|
|References||Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11788.|
|Structure formula Image|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11788.|
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