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-150617
    Lartesertib
    Inhibitor 99.94%
    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.
    Lartesertib
  • 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-N0245
    Theaflavin-3-gallate
    99.89%
    Theaflavin-3-gallate, a black tea theaflavin monomer, is regarded as the biologically important active component of black tea and provides health benefits. Theaflavin-3-gallate acts as prooxidants and induces oxidative stress in the carcinoma cells. Theaflavin-3-gallate reacts directly with reduced glutathione (GSH) in a time- and concentration-dependent manner. Theaflavin-3-gallate induces apoptosis and G1 cell cycle arrest in ovarian cancer A2780/CP70 cells through p53-dependent pathways. Theaflavin-3-gallate induces DNA damage through ATM/Chk/p53 pathway.
    Theaflavin-3-gallate
  • HY-15520
    CGK733
    Inhibitor 99.71%
    CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.
    CGK733
  • HY-B0255
    Adefovir dipivoxil
    Activator 99.03%
    Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer.
    Adefovir dipivoxil
  • HY-15521
    ETP-46464
    Inhibitor 99.54%
    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 99.51%
    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-103241
    Ro 90-7501
    Inhibitor 98.50%
    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-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-159480
    AD1058
    Inhibitor 98.11%
    AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC50: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases.
    AD1058
  • 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-P10280
    ATR kinase substrate peptide
    Substrate 99.30%
    ATR kinase substrate peptide (ASELPASQPQPFSAKKK) is a peptide substrate for ATR protein kinase and can be used to detect ATR kinase activity.
    ATR kinase substrate peptide
  • HY-162471
    GSK_WRN3
    98.54%
    GSK_WRN3 is selective WRN helicase inhibitor (pIC50 = 8.6). SK_WRN3 can selectively inhibit the growth of microsatellite unstable (MSI) cancer cells, induce DNA damage, and cause cell cycle arrest. GSK_WRN3 has anti-tumor activity.
    GSK_WRN3
  • HY-163944
    LL-K12-18
    Modulator 98.42%
    LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer.
    LL-K12-18
  • HY-19323A
    (S)-Ceralasertib
    Inhibitor 99.97%
    (S)-Ceralasertib ((S)-AZD6738) is the S-enantiomer of Ceralasertib (HY-19323). (S)-Ceralasertib is the inhibitor for ataxia telangiectasia mutated and rad3 related (ATR).
    (S)-Ceralasertib
  • HY-157764
    PROTAC ATR degrader-1
    Degrader 98.03%
    PROTAC ATR degrader-1 (compound ZS-7) is a potent PROTAC degrader of ataxia telangiectasia and Rad3-related (ATR), with DC50 of 0.53 μM. PROTAC ATR degrader-1 plays an importnt role in cancer research.
    PROTAC ATR degrader-1
  • HY-161615
    PROTAC ATR degrader-2
    Degrader 99.73%
    PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC50 of 29.6 nM against ATR, and its IC50 values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia.
    PROTAC ATR degrader-2
  • HY-112198
    AZ31
    Inhibitor 98.22%
    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-13816
    NU6027
    Inhibitor 98.01%
    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-162002
    WSD0628
    Inhibitor 99.43%
    WSD0628 is a brain penetrant and potent ATM inhibitor with profound radiosensitizing effect.
    WSD0628
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