1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  3. ATM/ATR

ATM/ATR

Ataxia telangiectasia mutated; ATM and RAD3 related

ATM/ATR, members of the phosphatidyl inositol 3-kinase-like family of serine/threonine protein kinases (PIKKs), are widely known as being central players in the mitotic DNA damage response (DDR), mounting responses to DNA double-strand breaks (DSBs) and single-stranded DNA (ssDNA) respectively. Activation of ATM by ionizing radiation results in the activation of signal transduction pathways that induce cell cycle arrest at G1/S, S and G2/M. ATR is required for cell cycle arrest in response to DNA-damaging agents such as ultraviolet radiation that cause bulky lesions.

Upon activation, ATM/ATR phosphorylate numerous targets to stabilize stalled replication forks, repair damaged DNA, and inhibit cell cycle progression to ensure survival of the cell and safeguard integrity of the genome. ATM and ATR are central players in activating cell cycle checkpoints and function as an active barrier against genome instability and tumorigenesis in replicating cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P10280
    ATR kinase substrate peptide
    Inhibitor 99.17%
    ATR kinase substrate peptide (compound 45) is a potent and selective inhibitor of ATR (Ataxia Telangiectasia and Rad3 related) protein kinase (Ki=6 nM). ATR kinase substrate peptide inhibits ATR activity by competing with ATR kinase ATP-binding sites to block ATR mediated signaling. ATR kinase substrate peptide can be used to study the role of ATR kinase in DNA damage response.
    ATR kinase substrate peptide
  • HY-18650
    KU 59403
    Inhibitor 99.23%
    KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
    KU 59403
  • HY-145312
    ATR-IN-4
    Inhibitor 98.35%
    ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13).
    ATR-IN-4
  • HY-101566S
    Elimusertib-d3
    Inhibitor 98.94%
    Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity.
    Elimusertib-d<sub>3</sub>
  • HY-157764
    PROTAC ATR degrader-1
    Degrader 98.02%
    PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research.
    PROTAC ATR degrader-1
  • HY-136835
    GJ071 oxalate
    Activator 99.74%
    GJ071 oxalate induces ATM kinase activity in ataxia telangiectasia (A-T) cells carrying homozygous TGA or TAG stop codons.
    GJ071 oxalate
  • HY-162002A
    (S)-WSD0628
    Inhibitor 99.84%
    (S)-WSD0628 (Compound 28) is the S-isomer of WSD0628 (HY-162002). (S)-WSD0628 is the inhibitor for ATM that inhibits the phosphorylation of ATM in MCF-7 cell with IC50 <100 nM. (S)-WSD0628 exhibits radiosensitizing activity. (S)-WSD0628 can cross blood-brain barrier.
    (S)-WSD0628
  • HY-145450
    ATR-IN-9
    Inhibitor
    ATR-IN-9 is a potent inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR) extracted from patent WO2020087170A1, compound 59, has an IC50 of 10 nM.
    ATR-IN-9
  • HY-112614
    ATM Inhibitor-1
    Inhibitor
    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
    ATM Inhibitor-1
  • HY-147566
    ATR-IN-14
    Inhibitor
    ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC50 of 64 nM.
    ATR-IN-14
  • HY-118911
    ATM Inhibitor-10
    Inhibitor
    ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors.
    ATM Inhibitor-10
  • HY-153462
    ATR-IN-24
    Inhibitor
    ATR-IN-24 (Compound 1) is a ATR inhibitor. ATR-IN-24 has anticancer activity.
    ATR-IN-24
  • HY-144686
    ATM Inhibitor-3
    Inhibitor
    ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability.
    ATM Inhibitor-3
  • HY-142672
    ATR-IN-6
    ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22).
    ATR-IN-6
  • HY-149952
    ATR-IN-23
    Inhibitor
    ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers.
    ATR-IN-23
  • HY-149291
    ATM Inhibitor-7
    Inhibitor
    ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity.
    ATM Inhibitor-7
  • HY-144687
    ATM Inhibitor-4
    Inhibitor
    ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability.
    ATM Inhibitor-4
  • HY-169209
    CA-M11
    Inhibitor
    CA-M11 (compund CA-M11) can enter the liver area of bile salt transport and release Mirin.
    CA-M11
  • HY-161616
    ATR-IN-30
    ATR-IN-30 is a selective ATR ligand, and can be used for synthesis of ATR PROTACs, such as PROTAC ATR degrader-2 (HY-161615).
    ATR-IN-30
  • HY-161838
    ICT10336
    Inhibitor
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
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