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, 2024, 10.1038/s41587-024-02172-9
-
Nat Metab, 2024, 6(2):323-342
-
J Biomed Sci, 2024, 31(1):90
|
|
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. |
-
EMBO J, 2024, 10.1038/s44318-024-00240-z
-
J Neuroinflammation, 2024, 21(1):57
-
Front Immunol, 2024, 15:1374943
|
|
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. |
-
Clin Transl Med, 2024, 14(2):e1567
-
Cell Rep, 2024, 43(11):114964
-
Acta Pharmacol Sin, 2024, 10.1038/s41401-023-01219-y
|
|
S7030 |
RG-7112
|
RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. |
-
Int J Mol Sci, 2024, 25(7)3948
-
bioRxiv, 2024, 2024.10.09.617493
-
Biomolecules, 2023, 13(8)1257
|
|
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. |
-
Genes Environ, 2024, 46(1):10
-
Transl Oncol, 2023, 35:101712
-
PLoS Genet, 2021, 17(11):e1009890
|
|
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. |
-
Nat Commun, 2024, 15(1):1391
-
J Exp Clin Cancer Res, 2024, 43(1):248
-
Mol Cells, 2024, 47(7):100079
|
|
S7649 |
MI-773 (SAR405838)
|
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
|
-
Pharmaceutics, 2023, 15(4)1274
-
Haematologica, 2022, 10.3324/haematol.2022.280879
-
Oncogenesis, 2022, 11(1):37
|
|
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. |
-
PLoS One, 2024, 19(1):e0295629
-
Front Oncol, 2021, 11:582511
-
Genes Dev, 2020, 34(7-8):526-543
|
|
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. |
-
Haematologica, 2022, 10.3324/haematol.2022.280879
-
Cell Death Dis, 2021, 12(1):98
-
Eur J Cancer, 2020, 126:93-103
|
|
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. |
-
J Exp Clin Cancer Res, 2023, 42(1):9
-
BMC Cancer, 2023, 23(1):47
-
Mol Cancer Ther, 2022, 21(11):1689-1700
|
|
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. |
-
Life Sci Alliance, 2022, 5(4)e202101157
-
Electrophoresis, 2015, 36(24):3101-4
|
|
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. |
-
Cell Death Dis, 2024, 15(9):662
-
Cells, 2021, 10(4)742
|
|
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
|
|
S8546New |
Alrizomadlin
|
Alrizomadlin(APG-115, AA-115) is a highly potent and efficacious inhibitor of MDM2 and binds to MDM2 with IC50 of 3.8 nM. It exhibits potent antiproliferative and apoptogenic activities and also significantly reduces tumor burden and prolonged survival in AML xenograft models. |
|
|
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. |
|
|
E1537 |
MMRi62
|
MMRi62 is a ferroptosis inducer, targeting MDM2-MDM4 with Kd value of 1.39 μM. It exhibits a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. |
|
|
S8703New |
Milademetan (DS-3032b)
|
Milademetan(RAIN-32, DS-3032) is an oral, selective inhibitor of the MDM2-p53 complex that reactivates p53 to induce cancer cell apoptosis and exhibits an anti-tumor effect. |
|
|
S7426New |
AMG 232 ( KRT-232 )
|
AMG 232 (Navtemadlin) is a potential, selective inhibitor of the MDM2–p53 interaction, with an IC50 of 0.6 nM and binds to MDM2 with a Kd of 0.045 nM. It also demonstrated antitumor activity in vivo in a variety of tumor types with different genetic backgrounds. |
|
|
E1491New |
Brigimadlin
|
Brigimadlin(BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. Brigimadlin inhibits MDM-2's suppression of the tumor suppressor p53. It promotes apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells. |
|
|
S6900New |
MD-224
|
MD-224 is a highly potent and effective degrader of the Human murine double minute 2 (MDM2) protein, the main cellular inhibitor of the tumor suppressor p53. It strongly inhibits cell growth in leukemia cell lines with wild-type p53 and induces complete and lasting tumor regression in the RS4;11 xenograft tumor model. |
|
|
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. |
|
|
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. |
- EMBO J, 2024, 10.1038/s44318-024-00240-z
- J Neuroinflammation, 2024, 21(1):57
- Front Immunol, 2024, 15:1374943
|
|
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. |
- Clin Transl Med, 2024, 14(2):e1567
- Cell Rep, 2024, 43(11):114964
- Acta Pharmacol Sin, 2024, 10.1038/s41401-023-01219-y
|
|
S7030 |
RG-7112
|
RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. |
- Int J Mol Sci, 2024, 25(7)3948
- bioRxiv, 2024, 2024.10.09.617493
- Biomolecules, 2023, 13(8)1257
|
|
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. |
- Nat Commun, 2024, 15(1):1391
- J Exp Clin Cancer Res, 2024, 43(1):248
- Mol Cells, 2024, 47(7):100079
|
|
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. |
- PLoS One, 2024, 19(1):e0295629
- Front Oncol, 2021, 11:582511
- Genes Dev, 2020, 34(7-8):526-543
|
|
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. |
- Haematologica, 2022, 10.3324/haematol.2022.280879
- Cell Death Dis, 2021, 12(1):98
- Eur J Cancer, 2020, 126:93-103
|
|
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. |
- J Exp Clin Cancer Res, 2023, 42(1):9
- BMC Cancer, 2023, 23(1):47
- Mol Cancer Ther, 2022, 21(11):1689-1700
|
|
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. |
- Cell Death Dis, 2024, 15(9):662
- Cells, 2021, 10(4)742
|
|
S8546New |
Alrizomadlin
|
Alrizomadlin(APG-115, AA-115) is a highly potent and efficacious inhibitor of MDM2 and binds to MDM2 with IC50 of 3.8 nM. It exhibits potent antiproliferative and apoptogenic activities and also significantly reduces tumor burden and prolonged survival in AML xenograft models. |
|
|
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. |
|
|
E1537 |
MMRi62
|
MMRi62 is a ferroptosis inducer, targeting MDM2-MDM4 with Kd value of 1.39 μM. It exhibits a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. |
|
|
S8703New |
Milademetan (DS-3032b)
|
Milademetan(RAIN-32, DS-3032) is an oral, selective inhibitor of the MDM2-p53 complex that reactivates p53 to induce cancer cell apoptosis and exhibits an anti-tumor effect. |
|
|
S7426New |
AMG 232 ( KRT-232 )
|
AMG 232 (Navtemadlin) is a potential, selective inhibitor of the MDM2–p53 interaction, with an IC50 of 0.6 nM and binds to MDM2 with a Kd of 0.045 nM. It also demonstrated antitumor activity in vivo in a variety of tumor types with different genetic backgrounds. |
|
|
E1491New |
Brigimadlin
|
Brigimadlin(BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. Brigimadlin inhibits MDM-2's suppression of the tumor suppressor p53. It promotes apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells. |
|
|
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. |
|
|