MTH1

MTH1 inhibitors and degraders target nudix hydrolase 1 (NUDT1, also called MTH1), which removes oxidized nucleotides. MTH1 hydrolyzes oxidized precursors such as 8-oxo-2'-deoxyguanosine triphosphate (8-oxo-dGTP), which keeps them out of newly synthesized DNA. In 2014 TH588 and TH287 were introduced as MTH1 inhibitors that increase oxidative damage in cancer cell DNA. A second 2014 study showed that (S)-crizotinib, the enantiomer of the anaplastic lymphoma kinase (ALK) inhibitor crizotinib, binds MTH1 stereospecifically. Later selective inhibitors such as BAY-707 and IACS-4619 were used to reexamine whether MTH1 inhibition alone reduces cancer cell survival. SU0383 inhibits both MTH1 and 8-oxoguanine DNA glycosylase 1 (OGG1). aTAG 4531 and aTAG 2139 are MTH1-binding degraders used to remove MTH1-tagged fusion proteins in targeted degradation studies.

4 Items

  • aTAG 4531
    Cat. No.
    A38067

    aTAG 4531

    Synonyms: CFT-4531

    aTAG 4531 is a selective MTH1 degrader that exerts its action through the formation of a ternary complex with MTH1, CRBN E3 ligase, and the degrader itself. It displays a DC50 value of 0.28 nM and a Ki value of 1.8 nM, highlighting its potent degradation capability. This compound is valuable for research focused on MTH1 inhibition and subsequent cellular effects, offering insights into its role in cancer biology and related therapeutic applications.

    1 mg
    $325.00
    5 mg
    $970.00
    All 2 sizes
  • aTAG 2139
    Cat. No.
    A38361

    aTAG 2139

    Synonyms: CFT-2139

    aTAG 2139 is a selective degrader targeting MTH1 via an aTAG-based mechanism. It demonstrates biological activity with a DC50 value of 1.1 nM and a Ki value of 2.1 nM for MTH1 inhibition. This compound is suitable for studies investigating the role of MTH1 in various cellular processes and therapeutic applications in cancer research.

    1 mg
    $285.00
    5 mg
    $870.00
    All 2 sizes
  • MTH1 degrader-1
    Cat. No.
    A38450

    MTH1 degrader-1

    MTH1 degrader-1 is a potent degrader targeting MTH1 through a PROTAC mechanism. This compound facilitates the selective degradation of MTH1, making it a valuable tool for studying the role of MTH1 in cancer metabolism and therapy resistance. Key applications include the development of PROTACs and the synthesis of related compounds, such as PROTAC aTAG 4531.

    Out of stock

    All 3 sizes
  • 8-Oxo-dGTP
    Cat. No.
    A39260

    8-Oxo-dGTP

    Synonyms: 8-Oxo-Deoxyguanosine triphosphate

    8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is a reactive oxidized guanine nucleotide that serves as a substrate for MTH1 and other pyrophosphohydrolases. This compound is known to act as a mutagen, integrating into DNA and leading to A:T to C:G transversions, which can contribute to genomic instability. Additionally, 8-Oxo-dGTP can provoke oxidative DNA modifications, strand breaks, and the promotion of apoptosis, particularly in mth1-deficient organisms. Its accumulation is linked to various biological processes and is extensively utilized in research on carcinogenesis, neurodegenerative diseases, and other pathologies.

    Out of stock

    All 3 sizes

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