MDM2/MDMX

MDM2/MDMX製品

• All (21)
• MDM2/MDMX阻害剤 (15)
• MDM2/MDMX活性剤(1)
• MDM2/MDMX拮抗剤(4)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	J Clin Invest, 2024, 134(15)e171136 Clin Transl Med, 2024, 14(2):e1567 Cell Rep, 2024, 43(11):114964
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. 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, 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.
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.	J Clin Invest, 2024, 134(15)e171136 Clin Transl Med, 2024, 14(2):e1567 Cell Rep, 2024, 43(11):114964
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. 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, 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.
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.
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
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
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
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
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.
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.