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-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, 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 (Standard)
  • HY-150617A
    (Rac)-Lartesertib
    Inhibitor
    (Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity.
    (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-118911A
    ATM-IN-12
    Inhibitor
    ATM-IN-12 (example 1.1) is an ATM kinase inhibitor with an IC50 of 1.26 μM. ATM-IN-12 can be used for the study of ATM kinase mediated disease, including cancer.
    ATM-IN-12
  • HY-182016
    PROTAC ATR degrader-3
    Degrader
    PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
    PROTAC ATR degrader-3
  • 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-13902A
    Berzosertib hydrochloride
    Inhibitor
    Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer.
    Berzosertib hydrochloride
  • HY-174989
    ATM-IN-2
    Inhibitor
    ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer.
    ATM-IN-2
  • HY-181786
    ATM-IN-13
    Inhibitor
    ATM-IN-13 (A36) is an orally active, selective ATM kinase inhibitor with a human IC50 of 0.3 nM. ATM-IN-13 blocks the ATM-mediated DNA double-strand break repair signaling pathway, reduces the phosphorylation levels of ATM and p53, and inhibits ATM-dependent DNA damage response. ATM-IN-13 can be used in the research of colorectal cancer.
    ATM-IN-13
  • 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
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