Mdm2

Choose Selective Mdm2 Inhibitors

Mdm2 Signaling Pathway Map

Mdm2 Signaling Pathways
Isoform-selective Inhibitors

Mdm2 Products

  • All (14)
  • Mdm2 Inhibitors (9)
  • Mdm2 Activators (1)
  • Mdm2 Antagonists (4)
  • New Mdm2 Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
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.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) 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.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
Nat Commun, 2021, 12(1):4019
Cells, 2021, 10(4)742
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S7205 Idasanutlin (RG-7388) Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
Nat Commun, 2021, 12(1):4019
Acta Neuropathol Commun, 2021, 9(1):178
Blood Adv, 2021, bloodadvances.2021006156
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.
Cell Death Dis, 2021, 12(1):98
Eur J Cancer, 2020, 126:93-103
Viruses, 2019, 11(8)
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.
PLoS Biol, 2021, 19(8):e3001364
Cell Death Dis, 2021, 12(7):663
Cell Death Dis, 2021, 12(4):364
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.
Cells, 2021, 10(4)742
S8606 HDM201 (Siremadlin) HDM201 (Siremadlin, NVP-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.
Eur J Cancer, 2020, 126:93-103
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.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
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.
Nat Cell Biol, 2021, 23(6):595-607
Sci Adv, 2021, 7(32)eabf7561
Nat Commun, 2021, 12(1):3481
S7489 YH239-EE YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
Cell Stem Cell, 2018, 23(4):544-556
S7649 MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Cell Rep, 2021, 36(5):109482
NPJ Precis Oncol, 2021, 5(1):96
Cancers (Basel), 2020, 12(8):E2157
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.
Electrophoresis, 2015, 36(24):3101-4
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.
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.
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
Sci Rep, 2019, 9(1):1897
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) 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.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
Nat Commun, 2021, 12(1):4019
Cells, 2021, 10(4)742
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S7205 Idasanutlin (RG-7388) Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
Nat Commun, 2021, 12(1):4019
Acta Neuropathol Commun, 2021, 9(1):178
Blood Adv, 2021, bloodadvances.2021006156
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.
Cell Death Dis, 2021, 12(1):98
Eur J Cancer, 2020, 126:93-103
Viruses, 2019, 11(8)
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.
PLoS Biol, 2021, 19(8):e3001364
Cell Death Dis, 2021, 12(7):663
Cell Death Dis, 2021, 12(4):364
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.
Cells, 2021, 10(4)742
S8606 HDM201 (Siremadlin) HDM201 (Siremadlin, NVP-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.
Eur J Cancer, 2020, 126:93-103
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.
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
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.
Nat Cell Biol, 2021, 23(6):595-607
Sci Adv, 2021, 7(32)eabf7561
Nat Commun, 2021, 12(1):3481
S7489 YH239-EE YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
Cell Stem Cell, 2018, 23(4):544-556
S7649 MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Cell Rep, 2021, 36(5):109482
NPJ Precis Oncol, 2021, 5(1):96
Cancers (Basel), 2020, 12(8):E2157
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.
Electrophoresis, 2015, 36(24):3101-4