ATM/ATR

ATM and ATR inhibitors act on ataxia telangiectasia mutated (ATM) and ATM and Rad3-related (ATR) kinases. The ATM gene was cloned in 1995 and encodes a protein similar to phosphatidylinositol 3-kinase (PI3K). ATR was cloned in 1996 as a candidate human cell cycle checkpoint protein. ATM responds mainly to DNA double-strand breaks, whereas ATR is activated by stalled replication forks. KU-55933, described in 2004 as a specific ATM inhibitor, is joined by KU-60019 and AZD0156. Ceralasertib, VE-821 and BAY-1895344 inhibit ATR and are used to study replication stress. Broader inhibitors of PI3K-related kinases, such as wortmannin, also appear in this list. Inhibitors of DNA-dependent protein kinase are listed in the sibling category DNA-PK.

3 Items

  • PROTAC ATR degrader-2
    Cat. No.
    A30914

    PROTAC ATR degrader-2

    PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia.

    5 mg
    $460.00
    10 mg
    $755.00
    All 4 sizes
  • PROTAC ATR degrader-1
    Cat. No.
    A54081

    PROTAC ATR degrader-1

    PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies.

    5 mg
    $740.00
    10 mg
    $1,220.00
    All 3 sizes
  • Abd110
    Cat. No.
    A54086

    Abd110

    Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage.

    1 mg
    $470.00
    5 mg
    $1,215.00
    All 6 sizes

3 Items

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