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-111783
    AZD-7648
    Inhibitor 99.86%
    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.
    AZD-7648
  • HY-19323
    Ceralasertib
    Inhibitor 99.76%
    Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
    Ceralasertib
  • HY-12016
    KU-55933
    Inhibitor 99.92%
    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.
    KU-55933
  • HY-12061
    KU-60019
    Inhibitor 99.43%
    KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.
    KU-60019
  • HY-109566
    AZD1390
    Inhibitor 99.28%
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell.
    AZD1390
  • 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-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
  • 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.
    Elimusertib
  • 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.
    VE-821
  • HY-100016
    AZD0156
    Inhibitor 99.83%
    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.
    AZD0156
  • 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.
    Camonsertib
  • HY-13902
    Berzosertib
    Inhibitor 99.70%
    Berzosertib (VE-822) is an ATR inhibitor with a Ki value of less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.
    Berzosertib
  • HY-117693
    Mirin
    Inhibitor 98.12%
    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.
    Mirin
  • HY-15557
    AZ20
    Inhibitor 99.40%
    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).
    AZ20
  • HY-123834
    FEN1-IN-1
    Activator 99.50%
    FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers.
    FEN1-IN-1
  • HY-136270
    Gartisertib
    Inhibitor 99.76%
    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.
    Gartisertib
  • HY-111451
    Tuvusertib
    Inhibitor 99.77%
    Tuvusertib (M1774; ATR inhibitor 1) is a selective and orally active ATR inhibitor extracted from patent WO2015187451A1, compound I-l, with a Ki value below 1 μΜ.
    Tuvusertib
  • HY-101566A
    Elimusertib hydrochloride
    Inhibitor 99.85%
    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.
    Elimusertib hydrochloride
  • HY-150617
    Lartesertib
    Inhibitor 99.89%
    Lartesertib (M4076) is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1).
    Lartesertib
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