MDM2/MDMX

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MDM2/MDMX Signaling Pathway Map

MDM2/MDMX Signaling Pathways
Isoform-selective Inhibitors

MDM2/MDMX Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E0051 SJ-172550 SJ 172550 is the first MDMX inhibitor that binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.
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.
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.
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.
Front Oncol, 2021, 11:582511
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
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.
Kidney Int, 2022, S0085-2538(22)00369-6
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
iScience, 2022, 25(6):104481
Phytomedicine, 2022, 98:153963
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
Blood Adv, 2022, 6(3):891-901
Front Pharmacol, 2022, 13:871259
Front Genet, 2022, 13:913030
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Adv Sci (Weinh), 2022, e2201539
Adv Sci (Weinh), 2022, e2200742
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.
Cancers (Basel), 2021, 14(1)14
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 Biotechnol, 2022, 10.1038/s41587-021-01172-3
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
J Exp Clin Cancer Res, 2022, 41(1):79
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.
Oncogenesis, 2022, 11(1):37
Cell Rep, 2021, 36(5):109482
Oncol Lett, 2021, 22(6):838
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
E0051 SJ-172550 SJ 172550 is the first MDMX inhibitor that binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.
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.
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.
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.
Front Oncol, 2021, 11:582511
Genes Dev, 2020, 34(7-8):526-543
Oncotarget, 2020, 11(46):4224-4242
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.
Kidney Int, 2022, S0085-2538(22)00369-6
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
S7030 RG-7112 RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.
iScience, 2022, 25(6):104481
Phytomedicine, 2022, 98:153963
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
Blood Adv, 2022, 6(3):891-901
Front Pharmacol, 2022, 13:871259
Front Genet, 2022, 13:913030
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Adv Sci (Weinh), 2022, e2201539
Adv Sci (Weinh), 2022, e2200742
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.
Cancers (Basel), 2021, 14(1)14
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 Biotechnol, 2022, 10.1038/s41587-021-01172-3
Cell Death Differ, 2022, 10.1038/s41418-022-00992-3
J Exp Clin Cancer Res, 2022, 41(1):79
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.
Oncogenesis, 2022, 11(1):37
Cell Rep, 2021, 36(5):109482
Oncol Lett, 2021, 22(6):838
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
Tags: MDM2/MDMX inhibitor|MDM2/MDMX agonist|MDM2/MDMX activator|MDM2/MDMX inducer|MDM2/MDMX antagonist|MDM2/MDMX signaling pathway|MDM2/MDMX assay kit