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).

5 Items

  • 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 carboxylic acid
    Cat. No.
    A18917

    Nutlin carboxylic acid

    Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid (MDM2 ligand 1) can be connected to the ligand for protein by a linker to form PROTACs.

    1 mg
    $120.00
    2 mg
    $235.00
    All 7 sizes
  • Seldegamadlin
    Cat. No.
    A30156

    Seldegamadlin

    Synonyms: KT-253

    Seldegamadlin is a selective p53 stabilizer and an MDM2 PROTAC degrader with a DC50 of 0.4 nM. It effectively inhibits the proliferation of RS4;11 cancer cells, demonstrating an IC50 of 0.3 nM, and induces cell cycle arrest at the G2/M phase while promoting apoptosis. By upregulating p53 activity, Seldegamadlin overcomes the p53-MDM2 feedback loop, making it a valuable tool for research in hematologic and solid tumors, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL).

    1 mg
    $335.00
    5 mg
    $765.00
    All 6 sizes
  • MDM2 ligand 5
    Cat. No.
    A53803

    MDM2 ligand 5

    MDM2 Ligand 5 is a potent ligand targeting the MDM2 protein, known for its role in regulating p53 activity. This compound serves as a critical building block for the development of Proteolysis Targeting Chimeras (PROTACs), facilitating the selective degradation of MDM2 to enhance p53-mediated tumor suppression. MDM2 Ligand 5 is valuable for research applications focused on cancer therapeutics and the modulation of oncogenic pathways.

    5 mg
    $245.00
    10 mg
    $405.00
    All 5 sizes
  • (rel)-Nutlin carboxylic acid
    Cat. No.
    A80605

    (rel)-Nutlin carboxylic acid

    (rel)-Nutlin carboxylic acid is an MDM2 ligand derived from Nutlin 3, targeting the MDM2 protein to inhibit its interaction with p53. This compound plays a crucial role in cancer research, particularly in the study of p53 pathway modulation and potential therapeutic interventions. It can also be utilized in the development of PROTACs when linked to other proteins, facilitating targeted protein degradation.

    Out of stock

    All 3 sizes

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