444153 Sigma-AldrichMDM2/MDMX Dual Inhibitor, RO-5963 - Calbiochem
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
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Overview
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| Description | |
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| Overview | This product has been discontinued. 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. |
| Catalogue Number | 444153 |
| Brand Family | Calbiochem® |
| 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 |
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| References | Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11788. |
| Product Information | |
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| Form | Orange-brown solid |
| Hill Formula | C₂₄H₂₁ClF₂N₄O₅ |
| Chemical formula | C₂₄H₂₁ClF₂N₄O₅ |
| Hygroscopic | Hygroscopic |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
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| Biological Information | |
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| Primary Target | MDMX |
| Secondary target | MDM2 |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Catalogue Number | GTIN |
| 444153 | 0 |
Documentation
MDM2/MDMX Dual Inhibitor, RO-5963 - Calbiochem SDS
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MDM2/MDMX Dual Inhibitor, RO-5963 - Calbiochem Certificates of Analysis
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| 444153 |
References
| Reference overview |
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| Graves, B., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 11788. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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