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

ATM/ATR

Ataxia telangiectasia mutated; ATM and RAD3 related

ATM/ATR

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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:

ATM/ATR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153400
    ATR-IN-22
    		Inhibitor
    ATR-IN-22 (Compound 34) is an orally active ATR inhibitor. ATR-IN-22 inhibits MIAPaCa-2 proliferation (IC50 <1 μM). ATR-IN-22 shows anti-tumor activity in colon cancer.
    ATR-IN-22
  • HY-N6954R
    Garcinone C (Standard)
    		Activator
    Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. 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, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time? and dose?dependent manner.
    Garcinone C (Standard)
  • HY-150617A
    (Rac)-Lartesertib
    		Inhibitor
    (Rac)-Lartesertib ((Rac)-M4076; (Rac)-ATM Inhibitor-5) is an isoform of Lartesertib (HY-150617), which is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1).
    (Rac)-Lartesertib
  • HY-144685
    ATM Inhibitor-2
    		Inhibitor
    ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM.
    ATM Inhibitor-2
  • HY-151915
    ATR-IN-20
    		Inhibitor
    ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.
    ATR-IN-20
  • HY-144436
    ATR-IN-12
    		Inhibitor
    ATR-IN-12 (Compound 5g) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with an IC50 value of 0.007 μM. ATR-IN-12 displays good anti-tumor activity and significantly reduces the phosphorylation level of ATR and its downstream signaling protein. ATR-IN-12 is a promising lead compound for subsequent agent discovery targeting ATR kinase.
    ATR-IN-12
  • HY-142924
    ATR-IN-8
    		Inhibitor
    ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3).
    ATR-IN-8
  • HY-144435
    ATR-IN-11
    		Inhibitor
    ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent agent discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease.
    ATR-IN-11
  • HY-141478
    Antitumor agent-28
    		Inhibitor
    Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.
    Antitumor agent-28
  • HY-153729
    ATR-IN-29
    		Inhibitor
    ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC50 value of 1 nM. ATR-IN-29 shows antiproliferative activity.
    ATR-IN-29
  • HY-147565
    ATR-IN-13
    		Inhibitor
    ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC50 of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer.
    ATR-IN-13
  • HY-136835
    GJ071 oxalate
    		Activator
    GJ071 oxalate induces ATM kinase activity in ataxia telangiectasia (A-T) cells carrying homozygous TGA or TAG stop codons.
    GJ071 oxalate
  • HY-147570
    ATR-IN-18
    		Inhibitor
    ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity.
    ATR-IN-18
  • HY-169930
    ATR kinase-IN-2
    		Inhibitor
    ATR kinase-IN-2 (Compound I-G-27) is a ATR protein kinase inhibitor with the Ki of 0.01 ~ 1 μΜ and can be used for study of cancer.
    ATR kinase-IN-2
  • HY-142671
    ATR-IN-5
    		Inhibitor
    ATR-IN-5 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-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24).
    ATR-IN-5
  • HY-155091
    ATM Inhibitor-9
    		Inhibitor
    ATM Inhibitor-9 (Compd 7a) is a potent ATM inhibitor with IC505 nM for ATM kinase, useful in cancer research.
    ATM Inhibitor-9
  • HY-155090
    ATM Inhibitor-8
    ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity.
    ATM Inhibitor-8
  • HY-169931
    ATR kinase-IN-3
    		Inhibitor
    ATR kinase-IN-3 (Compound I-G-28) is a ATR protein kinase inhibitor with the Ki of 0.01 ~ 1 μΜ and can be used for study of cancer.
    ATR kinase-IN-3
  • HY-147568
    ATR-IN-16
    		Inhibitor
    ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor. ATR-IN-16 shows good anticancer activity in LoVo cells, with an IC50 of 410 nM.
    ATR-IN-16
  • HY-123502
    Ceralasertib formate
    		Inhibitor
    Ceralasertib formate is a potent, selective and orally active ATR inhibitor with an IC50 value of 1 nM. Ceralasertib formate inhibits cell viability and induces DNA damage. Ceralasertib formate induces cell senescence. Ceralasertib formate shows antitumor activity.
    Ceralasertib formate
Cat. No. Product Name / Synonyms Application Reactivity
ATM/ATR Isoform Comparison

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