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.

ATM/ATR Isoform Specific Products:

Cat. No. Product Name Effect Purity
  • HY-19323
    Ceralasertib
    Inhibitor 99.00%
    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
  • HY-111783
    AZD-7648
    Inhibitor 99.89%
    AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.
  • HY-12016
    KU-55933
    Inhibitor 99.88%
    KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
  • HY-100016
    AZD0156
    Inhibitor 99.82%
    AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
  • HY-109566
    AZD1390
    Inhibitor 99.97%
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell.
  • HY-112198
    AZ31
    Inhibitor
    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.
  • 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.
  • 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.
  • HY-12061
    KU-60019
    Inhibitor 99.43%
    KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.
  • HY-101566A
    Elimusertib hydrochloride
    Inhibitor 99.84%
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas.
  • HY-14731
    VE-821
    Inhibitor 98.32%
    VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
  • HY-101566
    Elimusertib
    Inhibitor 99.99%
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.
  • HY-15557
    AZ20
    Inhibitor 99.86%
    AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
  • HY-136270
    Gartisertib
    Inhibitor 99.88%
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
  • HY-139609
    Camonsertib
    Inhibitor 99.75%
    Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.
  • HY-15520
    CGK733
    Inhibitor 99.83%
    CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.
  • HY-112305
    AZ32
    Inhibitor 99.62%
    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.
  • HY-117693
    Mirin
    Inhibitor 98.02%
    Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells.
  • HY-11002
    CP-466722
    Inhibitor 99.91%
    CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
  • HY-103241
    Ro 90-7501
    Inhibitor
    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.

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