| S7649 |
MI-773 (SAR405838) |
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
|
Selective |
MDM2, Ki: 0.88 nM; MDM2, Kd: 8.2 nM |
| 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. |
Selective |
MDM2, IC50: 1.7 nM |
| S0167 |
RO8994 |
RO8994 is a potent and selective small-molecule MDM2 inhibitor with IC50 values of 5 nM in HTRF binding assays and 20 nM in MTT proliferation assays, respectively. |
Selective |
MDM2, IC50: 5 nM; MDM2, IC50: 20 nM |
| S1061 |
Nutlin-3 |
Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells. |
Selective |
MDM2, IC50: 180 nM |
| S0901 |
SP141 |
SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner. |
Selective |
MDM2, IC50: <0.50 μM |
| S8403 |
MX69 |
MX69 is a MDM2/XIAP inhibitor that binds to MDM2 RING protein with binding Kd values of 2.34 μM. It is used for cancer treatment. |
Selective |
MDM2, Kd: 2.34 μM |
| S8065 |
Nutlin-3b |
Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a. |
Selective |
MDM2, IC50: 13.6 μM |
| S3604 |
Triptolide |
Triptolide is a diterpene triepoxide, immunosuppresive 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. |
Selective |
|
| S2341 |
(-)-Parthenolide |
(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions. |
Selective |
|
| S8606 |
Siremadlin (HDM201) |
Siremadlin (HDM201) is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4. |
Pan |
|
| S7205 |
Idasanutlin (RG7388) |
Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity. |
Pan |
p53-MDM2 interaction, IC50: 6 nM |
| S7030 |
RG-7112 |
RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. |
Pan |
MDM2, Kd: 11 nM; p53-MDM2 interaction, IC50: 18 nM |
| 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. |
Pan |
p53-MDM2 interaction, IC50: 90 nM |
| S7489 |
YH239-EE |
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
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Pan |
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