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Mdm2

Mouse double minute 2 homolog (MDM2) also known as E3 ubiquitin-protein ligase Mdm2 is a protein that in humans is encoded by the MDM2 gene. Mdm2 is an important negative regulator of the p53 tumor suppressor. Mdm2 protein functions both as an E3 ubiquitin ligase that recognizes the N-terminal trans-activation domain (TAD) of the p53 tumor suppressor and as an inhibitor of p53 transcriptional activation.

  • Alrizomadlin
    T143031818393-16-6
    Alrizomadlin (APG-115) is an orally active inhibitor of MDM2 with IC50 of 3.8 nM and Ki of 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
    • $263
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  • Navtemadlin
    TQ01271352066-68-2
    Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.
    • $67
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  • p53-Mdm2 inhibitor 4
    T67698350678-63-6
    p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.
    • $50
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  • RDR03871
    T28509286008-51-3In house
    RDR03871 is an MDM2 inhibitor.
    • $117
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  • Milademetan
    T120401398568-47-2In house
    Milademetan (DS-3032) is an orally active and potent MDM2 inhibitor with antitumor activity that induces G1 cell cycle arrest, senescence, and apoptosis.Milademetan is used in the study of acute myeloid leukemia and solid tumors.
    • $178
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  • RO-5963
    T167711416663-77-8In house
    RO-5963 is a dual inhibitor of p53-MDM2 and p53-MDMX (IC50s: ~17 nM and ~24 nM, respectively).
    • $106
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  • SAR405838
    T65851303607-60-4In house
    MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
    • $45
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  • Kevetrin hydrochloride
    T318466592-89-0
    Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
    • $38
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    TargetMol | Citations Cited
  • Nutlin-3b
    T6614675576-97-3
    Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
    • $35
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  • IVHD-valtrate
    TN434128325-56-6
    VHD-valtrate has anticancer effects against human ovarian cancer cells in vitro and in vivo, it is a potential therapeutic agent for ovarian cancer, providing a basis for development of the compound as a novel chemotherapeutic agent.
    • $2,998
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  • Ganoderic acid X
    TN410786377-53-9
    Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.
    • $290
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  • MG-277
    T12027
    MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.
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  • Idasanutlin
    T62541229705-06-9
    Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
    • $34
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  • PhiKan 083
    T16523L880813-36-5
    PhiKan 083 is a carbazole derivative
    • $30
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  • SJ-172550
    T16888431979-47-4
    SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).
    • $37
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  • RITA
    T1798213261-59-7
    RITA (NSC-652287)(NSC-652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53/Mdm2 interaction.
    • $30
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    TargetMol | Citations Cited
  • MI-1061
    T120311410737-34-6
    MI-1061 is a orally bioavailable inhibitor of MDM2 (MDM2-p53 interaction) (IC50=4.4 nM).
    • $3,598
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  • p53-MDM2-IN-1
    T72026381717-91-5
    p53-MDM2-IN-1 (Example 30), an inhibitor targeting the p53-MDM2/X protein interaction, exhibits a K i value of 23.35 µM. This compound holds potential for applications in anti-tumor research.
    • $195
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  • MA242
    T119311049704-18-8
    MA242 is a nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy and dual inhibitor of murine double minute 2 (MDM2).
    • $2,270
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  • Serdemetan
    T2243881202-45-5
    Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
    • $39
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    TargetMol | Citations Cited
  • UC2288
    T96981394011-91-6
    UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.
    • $41
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  • SP-141
    T217731253491-42-7
    SP 141 is a MDM2 inhibitor.SP-141 promotes MDM2 auto-ubiquitination and degradation, with anticancer activity.
    • $38
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  • XI-006
    T661058131-57-0
    XI-006 (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.
    • $51
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  • MD-224
    T119802136247-12-4
    MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.
    • $64
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  • RO8994
    T35171309684-94-3
    RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding assays).
    • $34
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  • Triptolide
    T217938748-32-2
    Triptolide (PG490) belongs to the tricyclic diterpenoid group of natural products and is an inhibitor of NF-κB activation. Triptolide exhibits immunosuppressive, anti-rheumatic, anti-inflammatory, anti-proliferative and anti-tumor activities.
    • $37
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  • NVP-CGM097
    TQ02311313363-54-0
    NVP-CGM097 (CGM097) is an effective and specific MDM2 inhibitor (IC50: 1.7 nM for hMDM2).
    • $79
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  • MX69
    T36531005264-47-0
    MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
    • $31
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  • RG7112
    T6965939981-39-2
    RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.
    • $41
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  • AM-8735
    T142031429386-01-5
    AM-8735 is an inhibitor of MDM2 ( IC50: 25 nM).
    • $1,820
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  • NSC 66811
    T215786964-62-1
    NSC 66811is a novel inhibitor of the murine double minute 2 (MDM2)-p53 interaction. It binds to MDM2 with a Ki of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction.
    • $30
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  • MMRi64
    T28078430458-66-5
    MMRi64 is a specific inhibitor of Mdm2-MdmX E3 ligase activity.MMRi64 potently induces p53 accumulation and apoptosis in the p53 pathway in leukemia/lymphoma cells, disrupts Mdm2-MdmX interactions, and downregulates Mdm2 and MdmX in leukemia cells.MMRi64 MMRi64 can be used in cancer research.
    • $51
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  • Tenovin-1
    T1919380315-80-0
    Tenovin-1 inhibits protein-deacetylating activities of SirT1 and SirT2 and protects against MDM2-mediated p53 degradation, which involves ubiquitination.
    • $50
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