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-112198
    AZ31
    Inhibitor 98.22%
    AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.
    AZ31
  • HY-P2096
    Hexapeptide-11
    Inhibitor 99.77%
    Hexapeptide-11 is an anti-aging peptide that can protect fibroblasts from premature cell senescence mediated by oxidative stress. Hexapeptide-11 is also a potential stimulator of hyaluronic acid in keratinocytes, and can enhance skin barrier function by upregulating the expression of HAS2 and EGR3, and downregulating the expression of HYAL2. Hexapeptide-11 can also improve skin elasticity.
    Hexapeptide-11
  • HY-160096
    M3541
    Inhibitor 99.28%
    M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities.
    M3541
  • HY-144217
    SKLB-197
    99.91%
    SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
    SKLB-197
  • HY-158345
    PROTAC ATM degrader-1
    Degrader 98.01%
    PROTAC ATM degrader-1 is a ATM PROTAC degrader with a KD value of 1.17 nM. PROTAC ATM degrader-1 triggers DNA damage response, cell cycle arrest, and apoptosis in cancer cells via the ubiquitin-proteasome-dependent degradation pathway. PROTAC ATM degrader-1 can be used for research on colorectal cancer.
    PROTAC ATM degrader-1
  • 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-118911
    ATM Inhibitor-10
    Inhibitor 98.7%
    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-N11709
    Theasaponin E1
    Activator 98.68%
    Theasaponin E1 is an orally effective tea saponin. Theasaponin E1 inhibits the proliferation of cancer cells by activating apoptosis. Theasaponin E1 inhibits angiogenesis in ovarian cancer cells and HUVECs by reducing the expression of VEGF. Theasaponin E1 upregulates the phosphorylation level of ATM protein and the expression level of PTEN protein in cancer cells, decreases the phosphorylation levels of Akt, mTOR, p70S6K and 4E-BP1 proteins, downregulates the expression of HIF-1α and NF-κB, and reduces the protein expression of Notch ligands Dll4 and Jagged1. Theasaponin E1 exerts neuroprotective effects by inhibiting the activity of acetylcholinesterase, activating α-secretase and neprilysin, reducing the concentration of , and inhibiting the activities of β-secretase and γ-secretase. Theasaponin E1 exhibits toxic effects on cancer cells and quinone reductase-inducing activity, and inhibits tumor growth in vivo. Theasaponin E1 induces ferroptosis in Pomacea canaliculata by synergistically disrupting cholesterol homeostasis and sphingolipid metabolism. Theasaponin E1 possesses anti-biofilm activity against Candida albicans. Theasaponin E1 can be used in the research of ovarian cancer, obesity, Alzheimer's disease and fungal infections.
    Theasaponin E1
  • 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-157767
    Abd110
    Inhibitor 98.67%
    Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs.
    Abd110
  • 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-172448
    YY2201
    Inhibitor
    YY2201 is a highly potent and selective ATR inhibitor with an IC50 of 8 nM. YY2201 shows >200-fold more selective for ATR than mTOR. YY2201 inhibits tumor progression in broad-spectrum cancer types (such as lung cancer).
    YY2201
  • 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-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-174828
    ATR/PARP1-IN-1
    Inhibitor
    ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change.
    ATR/PARP1-IN-1
Cat. No. Product Name / Synonyms Application Reactivity

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