MDM2

MDM2 inhibitors disrupt the binding of mouse double minute 2 homolog (MDM2) to the tumor suppressor p53. In 1992 the MDM2 protein was shown to form a complex with p53 and inhibit p53-mediated transactivation. MDM2 is also an E3 ubiquitin ligase that promotes the rapid degradation of p53, as reported in 1997. Nutlins, reported in 2004, occupy the p53-binding pocket of MDM2 and activate the p53 pathway in cells and in vivo. Nutlin 3a is the active enantiomer of nutlin-3, and Nutlin 3b is a much weaker enantiomer used as a control. RG7112 and APG-115 are further MDM2 inhibitors, while MD-224 is a degrader that removes MDM2 protein. SJ 172550 targets the MDM2 relative MDM4 (also called MDMX).

Items 1-25 of 91

  • Nutlin-3
    Cat. No.
    A10657

    Nutlin-3

    MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.

    2 mg
    $45.00
    5 mg
    $60.00
    All 7 sizes
  • Nutlin 3a
    Cat. No.
    A11501

    Nutlin 3a

    Synonyms: (-)-Nutlin-3

    Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.

    1 mg
    $40.00
    2 mg
    $55.00
    All 8 sizes
  • SJ 172550
    Cat. No.
    A15352

    SJ 172550

    SJ 172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.

    2 mg
    $30.00
    5 mg
    $50.00
    All 8 sizes
  • Minocycline hydrochloride
    Cat. No.
    A20954

    Minocycline hydrochloride

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.

    25 mg
    $30.00
    50 mg
    $45.00
    All 6 sizes
  • NSC-207895
    Cat. No.
    A11179

    NSC-207895 (XI-006)

    Synonyms: XI-006

    NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.

    1 mg
    $45.00
    2 mg
    $65.00
    All 9 sizes
  • Nutlin 3b
    Cat. No.
    A11502

    Nutlin 3b

    Synonyms: (+)-Nutlin-3

    Nutlin 3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 uM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

    1 mg
    $30.00
    2 mg
    $45.00
    All 8 sizes
  • RG7112
    Cat. No.
    A11523

    RG7112

    Synonyms: RO5045337

    RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.

    1 mg
    $35.00
    2 mg
    $50.00
    All 9 sizes
  • APG-115
    Cat. No.
    A12575

    APG-115

    APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively.

    1 mg
    $255.00
    5 mg
    $610.00
    All 7 sizes
  • MA242
    Cat. No.
    A13480

    MA242

    MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes
  • MDM2 Inhibitor
    Cat. No.
    A13582

    MDM2 Inhibitor

    MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex.

    10 mg
    $120.00
    25 mg
    $250.00
    All 4 sizes
  • Kevetrin HCl
    Cat. No.
    A13797

    Kevetrin HCl

    Synonyms: thioureidobutyronitrile

    Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

    5 mg
    $30.00
    10 mg
    $55.00
    All 7 sizes
  • AMG232
    Cat. No.
    A14394

    AMG232

    AMG 232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).

    1 mg
    $60.00
    2 mg
    $90.00
    All 7 sizes
  • MI-773 (SAR405838)
    Cat. No.
    A14423

    MI-773 (SAR405838)

    Synonyms: MI 773

    MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.

    5 mg
    $140.00
    10 mg
    $230.00
    All 4 sizes
  • WR 1065
    Cat. No.
    A15353

    WR 1065

    WR 1065, a dephosphorylated metabolite of amifostine (Ethyol), can protect against the immediate and delayed effects of radiation exposure.

    5 mg
    $25.00
    10 mg
    $35.00
    All 5 sizes
  • NVP-CGM097
    Cat. No.
    A16326

    NVP-CGM097

    Synonyms: CGM097

    NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity.

    1 mg
    $70.00
    2 mg
    $135.00
    All 8 sizes
  • MX-69
    Cat. No.
    A16348

    MX-69

    MX-69 is the MDM2/XIAP inhibitor, used for cancer treatment.

    1 mg
    $25.00
    2 mg
    $35.00
    All 9 sizes
  • HDM201
    Cat. No.
    A16834

    HDM201

    Synonyms: NVP-HDM201

    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.

    1 mg
    $55.00
    2 mg
    $70.00
    All 8 sizes
  • MI-1061
    Cat. No.
    A18450

    MI-1061

    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.

    1 mg
    $140.00
    5 mg
    $345.00
    All 6 sizes
  • RO-5963
    Cat. No.
    A18813

    RO-5963

    RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53 with IC50s of ~17 nM and ~24 nM, respectively.

    1 mg
    $55.00
    5 mg
    $200.00
    All 8 sizes
  • Milademetan
    Cat. No.
    A20456

    Milademetan

    Synonyms: DS-3032

    Mliademetan is a specific MDM2 inhibitor, a pharmaceutical composition for use in treating acute myeloid leukemia (AML).

    1 mg
    $170.00
    5 mg
    $540.00
    All 7 sizes
  • PK 11195
    Cat. No.
    A20724

    PK 11195

    Synonyms: RP 52028

    PK 11195 is a 2 Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitor, and is potentially useful for the Treatment of Gliomas.

    2 mg
    $25.00
    5 mg
    $50.00
    All 6 sizes
  • BI-0252
    Cat. No.
    A20824

    BI-0252

    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM.

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes

Items 1-25 of 91

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