MDM2/MDMX inhibitors/antagonists
Other Apoptosis Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S1061 | Nutlin-3 | Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with an IC50 of 90 nM in a cell-free assay; it stabilises p73 in p53-deficient cells. |
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| S7030 | RG-7112 | RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. |
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| S8059 | Nutlin-3a | Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner. |
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| E1491 | Brigimadlin | Brigimadlin (BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. This compound inhibits MDM-2's suppression of the tumour suppressor p53. It promotes Apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells. | ||
| S3604 | Triptolide | Triptolide is a diterpene triepoxide, an immunosuppressive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway. |
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| S7205 | Idasanutlin (RG7388) | Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with an IC50 of 6 nM, and it shows improved in vitro binding as well as cellular potency/selectivity. |
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| S7649 | SAR405838 | SAR405838 is an orally available MDM2 antagonist with Ki of 0.88 nM. This compound is a diastereomer of MI-773 (CAS: 1303607-07-9). Phase 1. |
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| S2678 | NSC 207895 | NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
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| S7875 | NVP-CGM097 | NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway. |
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| S8606 | Siremadlin (HDM201) | Siremadlin (HDM201) is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction, with an affinity constant for MDM2 in the picomolar range and a selectivity ratio greater than 10000-fold vs MDM4. |
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