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-19959
    (Z)-Mirin
    Inhibitor 99.63%
    (Z)-Mirin is an MRN (Mre11-Rad50-Nbs1) inhibitor. (Z)-Mirin prevents MRN-dependent activation of ATM without affecting ATM protein kinase activity. (Z)-Mirin inhibits Mre11-associated exonuclease activity. (Z)-Mirin increases apoptosis, triggers a G2/M checkpoint and strongly inhibits homology-directed repair (HDR).
    (Z)-Mirin
  • HY-15520
    CGK733
    Inhibitor 99.83%
    CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.
    CGK733
  • HY-11002
    CP-466722
    Inhibitor 99.74%
    CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
    CP-466722
  • HY-103241
    Ro 90-7501
    Inhibitor 99.10%
    Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces 42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
    Ro 90-7501
  • HY-15521
    ETP-46464
    Inhibitor 99.55%
    ETP-46464 is an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 nM, respectively.
    ETP-46464
  • HY-N6954
    Garcinone C
    Activator 99.66%
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.
    Garcinone C
  • HY-19323A
    (S)-Ceralasertib
    Inhibitor 98.84%
    (S)-Ceralasertib ((S)-AZD6738) is extracted from patent WO2011154737A1, Compound II, exhibits an IC50 of 2.578 nM. (S)-Ceralasertib is a potent and selective sulfoximine morpholinopyrimidine ATR inhibitor with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. (S)-Ceralasertib is developed improving aqueous solubility and eliminates CYP3A4 time-dependent inhibition.
    (S)-Ceralasertib
  • HY-159480
    AD1058
    Inhibitor 98.11%
    AD1058 is an orally active, selective, and blood-brain barrier permeable inhibitor of ATR. AD1058 exhibits in vivo anticancer activity, inhibiting cell proliferation, disrupting the cell cycle, and inducing Apoptosis. AD1058 can be utilized in research on brain and central nervous system metastases stemming from advanced solid tumors.
    AD1058
  • HY-112305
    AZ32
    Inhibitor 99.94%
    AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
    AZ32
  • HY-13816
    NU6027
    Inhibitor 99.04%
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
    NU6027
  • 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-P2096
    Hexapeptide-11
    Inhibitor 99.52%
    Hexapeptide-11 is a bioactive peptide with anti-aging effect. Hexapeptide-11 protects fibroblasts against oxidative stress-mediated premature cellular senescence by mediating a downregulation of cellular proteins, such as ataxia telangiectasia mutated (ATM) and p53 .
    Hexapeptide-11
  • HY-162472
    XRD-0394
    Inhibitor 98.54%
    XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.
    XRD-0394
  • HY-157941
    ART0380
    Inhibitor 99.89%
    ART0380 is a potent and selective ATR kinase inhibitor. ART0380 has selective antitumor activity that can be used for the research of Ataxia-Telangiectasia Mutated (ATM) aberrant cancers.
    ART0380
  • HY-112198
    AZ31
    Inhibitor 98.13%
    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-162002
    WSD0628
    Inhibitor 99.43%
    WSD0628 is a brain penetrant and potent ATM inhibitor with profound radiosensitizing effect.
    WSD0628
  • 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-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 99.17%
    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-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
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