MDM2 Activators
MDM2 activators are compounds that specifically enhance the activity of MDM2, a critical regulatory protein that controls the level and activity of the tumor suppressor protein p53. MDM2 (Murine Double Minute 2) is an E3 ubiquitin ligase that ubiquitinates p53, marking it for degradation by the proteasome, thus serving as a key negative regulator of p53. Under normal conditions, this interaction is crucial for maintaining low levels of p53, preventing unnecessary cell cycle arrest or apoptosis. MDM2 itself is regulated by feedback mechanisms and is subject to various post-translational modifications that affect its function. The activity of MDM2 is finely tuned, as its overactivity can lead to unchecked cell growth, while insufficient activity can cause excessive cell death or senescence. MDM2 activators influence this balance by promoting the MDM2-mediated ubiquitination of p53, effectively modulating the cellular concentration and activity of p53.
Chemically, MDM2 activators may belong to various structural classes and can act through different mechanisms to increase MDM2 activity. Some activators may bind directly to MDM2, stabilizing its structure or inducing conformational changes that increase its affinity for p53 or its ubiquitin ligase activity. Other activators might function by enhancing the interaction between MDM2 and its E2 ubiquitin-conjugating enzymes, thereby facilitating the transfer of ubiquitin to p53. Additionally, certain activators may increase the expression of MDM2 at the transcriptional level or inhibit the interaction of proteins that normally suppress MDM2's activity.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
(–)-Nutlin-3 | 675576-98-4 | sc-222086 sc-222086A | 1 mg 5 mg | $120.00 $215.00 | 2 | |
Nutlin-3 is a small molecule inhibitor that disrupts the interaction between MDM2 and p53. By binding to the p53-binding pocket of MDM2, nutlin-3 prevents MDM2-mediated degradation of p53, leading to the stabilization and activation of p53. This activation results in the transcription of p53 target genes involved in cell cycle arrest and apoptosis, indirectly influencing MDM2 activity by enhancing its regulatory interaction with p53. | ||||||
NSC-207895 | 58131-57-0 | sc-364550 sc-364550A | 5 mg 10 mg | $347.00 $653.00 | ||
NSC 207895 is a small molecule inhibitor that interferes with the interaction between MDM2 and ribosomal proteins. This disruption leads to the stabilization and activation of p53, as MDM2's association with ribosomal proteins is crucial for the regulation of p53 degradation. NSC 207895 indirectly influences MDM2 by targeting its interaction with ribosomal proteins, resulting in p53 activation and the subsequent transcriptional response. | ||||||
Pifithrin-α hydrobromide | 63208-82-2 | sc-45050 sc-45050A | 5 mg 25 mg | $118.00 $287.00 | 36 | |
Pifithrin-α(HBr) is a small molecule that inhibits the transcriptional activity of p53. While not directly targeting MDM2, pifithrin-α indirectly influences MDM2 by preventing p53-mediated transcriptional responses. By inhibiting the transcriptional activity of p53, pifithrin-α disrupts the downstream effects of p53 on MDM2 expression, influencing the cellular balance between MDM2 and p53. | ||||||