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PI3K/mTOR Inhibitor
BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.- Kohei Maruyama, .et al. , NPJ Precis Oncol, 2025, Jan 6;9(1):4 PMID: 39762482
- Lijuan Chen, .et al. , Behav Neurol, 2023, May 9;2023:6991826 PMID: 37200987
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. , FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. , Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
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ATM inhibitor
KU-55933 is an ATM inhibitor by suppressing cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt.- Ryo Sakasai, .et al. , Biochem Biophys Res Commun, 2023, Aug 6;668:42-48 PMID: 37244033
- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mariko Shikata, .et al. , Chem Res Toxicol, 2021, Dec 20;34(12):2512-2521 PMID: 34784199
- Masaya Igase, .et al. , Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- Hayakawa K, .et al. , Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
- Chwastek J, .et al. , Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
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ATM Inhibitor
KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
- Hegedus C, .et al. , Cancers (Basel), 2019, Dec 18;12(1) PMID: 31861350
- Masaya Igase, .et al. , Mol Ther Oncolytics, 2019, vol 15 PMID: 31650025
- CHENGHUA LOU, .et al. , Oncol Lett, 2016, Jul; 12(1): 295-300 PMID: 27347141
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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
- Weili Chen, .et al. , Communications Biology, 2024, 7:488
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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mTOR inhibitor
Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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ATM/ATR inhibitor
VE-821 is a potent and selective inhibitor of protein kinase ATR.- Yiovana Veronica Okraine, .et al. , Cell Death Dis, 2025, Jul 8;16(1):503 PMID: 40628724
- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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ATR inhibitor
Berzosertib (VE-822) is an potent ATR inhibitor.
- Joshua J Deppas, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117375
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ATR inhibitor
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
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ATR inhibitor
AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.- Joshua J Deppas, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117375
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Zhiyan Silvia Liu, .et al. , Cancer Res, 2024, Feb 15;84(4):577-597 PMID: 37967363
- Yang Lim, .et al. , Science, 2023, Sep 22;381(6664) PMID: 37590370
- Brian F Kiesel, .et al. , Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. , Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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ATM inhibitor
AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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ATR inhibitor
BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.- Joshua J Deppas, .et al. , Toxicol Appl Pharmacol, 2025, Jul:500:117375
- Brian F Kiesel, .et al. , Cancer Chemother Pharmacol, 2022, Jun;89(6):795-807 PMID: 35507041
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ATR inhibitor
ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 ?μ. -
ATM inhibitor
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM. -
ATR inhibitor
Gartisertib (VX-803, ATR inhibitor 2) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM.
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ATR inhibitor
Camonsertib is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays.
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ATR Inhibitor
AD1058 is a selective, orally active inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR) with an IC50 of 1.6 nM. This compound demonstrates significant anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis in various cancer models. AD1058 is particularly relevant for research focused on advanced malignancies and brain metastases, providing a valuable tool for investigating therapeutic strategies in these challenging areas. -
ATM Inhibitor
ATM Inhibitor-7 is a selective inhibitor of ataxia-telangiectasia mutated (ATM) with an IC50 of 1.0 nM. This compound effectively induces apoptosis and causes G2/M phase cell cycle arrest, particularly when combined with CPT-11. ATM Inhibitor-7 is utilized in research applications focused on elucidating mechanisms of tumor biology and enhancing the efficacy of chemotherapeutic agents. -
ATM Inhibitor
Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit the growth of various hematopoietic cell lines. Furthermore, in combination with the ATR inhibitor Tuvusertib, Lartesertib enhances tumor cell apoptosis and activates immune signaling pathways, showcasing significant anti-tumor efficacy. -
ATM Inhibitor
(Rac)-Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit cell proliferation in various hematopoietic cell lines. Moreover, when used in conjunction with the ATR inhibitor Tuvusertib, (Rac)-Lartesertib can enhance tumor cell death, activate immune signaling pathways, and exhibit notable anti-tumor efficacy, making it a valuable tool for cancer research. -
ATR Inhibitor
ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer. -
ATR Inhibitor
ATR-IN-31 is a selective ATR kinase inhibitor that exhibits an IC50 of 7 nM, demonstrating its potent activity. This compound functions by specifically inhibiting ATR kinase activity without significantly affecting ATM kinase. ATR-IN-31 has shown efficacy in reducing the viability of prostate cancer cells, making it a valuable tool for research focused on prostate cancer. -
ATM/ DNA-PKcs Inhibitor
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms. -
ATR Inhibitor
(S)-Ceralasertib is an ATR inhibitor, specifically targeting ataxia telangiectasia mutated and rad3 related (ATR) signaling pathways. This compound exhibits significant potential in cancer research by enhancing the sensitivity of tumor cells to DNA-damaging agents through inhibition of the ATR pathway. (S)-Ceralasertib is utilized in studies aimed at understanding the roles of DNA repair mechanisms and evaluating combination therapies for various cancers. -
ATM Inhibitor
WSD0628 is a potent ATM inhibitor known for its ability to cross the blood-brain barrier. It exhibits significant radiosensitizing effects, making it a valuable tool for research in cancer therapy and radiobiology. Its inhibition of the ATM pathway has implications for enhancing the efficacy of radiotherapy in various malignancies. -
ATM Inhibitor
M3541 is a potent, ATP-competitive inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 0.25 nM. This compound demonstrates significant selectivity against other protein kinases. M3541 effectively hinders the repair of double-strand breaks (DSB) and displays notable antitumor activity, making it a valuable tool for cancer research and therapeutic studies targeting DNA damage response pathways. -
ATR Inhibitor
ATR-IN-4 is a selective inhibitor of the ATR (Ataxia Telangiectasia Mutated and Rad3-related) kinase. This compound exhibits significant antiproliferative activity against human prostate cancer cells (DU145) and human lung cancer cells (NCI-H460), yielding IC50 values of 130.9 nM and 41.33 nM, respectively. ATR-IN-4 is valuable for research investigating DNA damage response pathways and potential therapeutic strategies in cancer treatment. -
Atm Inhibitor
ATM Inhibitor-10 is a selective ATM inhibitor characterized as a 3-quinoline carboxamide with an IC50 of 0.6 nM. This compound demonstrates significant anti-tumor activity in SW620 xenograft models and shows synergistic effects when combined with Top I inhibitors. It serves as a valuable tool for studies involving DNA damage response and cancer therapeutics. -
ATM Inhibitor
(S)-WSD0628 is a selective ATM inhibitor that effectively inhibits the phosphorylation of ATM in MCF-7 cells, with an IC50 of less than 100 nM. This compound demonstrates radiosensitizing properties, enhancing the efficacy of radiotherapy in cancer treatments. Additionally, (S)-WSD0628 is capable of crossing the blood-brain barrier, making it a valuable tool for research applications in neuro-oncology and other fields where central nervous system exposure is essential. -
ATR Inhibitor
ATR-IN-9 is a selective inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR), with an IC50 value of 10 nM, indicating its high potency. This compound is useful for research applications involving cell cycle regulation, DNA damage response, and cancer therapeutics, offering insights into the role of ATR in cellular processes. Its ability to modulate ATR activity makes it a valuable tool in studies focused on tumor biology and therapeutic resistance. -
ATR Inhibitor
ATR-IN-14 is a potent ATR kinase inhibitor that effectively disrupts ATR signaling pathways by inhibiting CHK1 protein phosphorylation, achieving 98.03% inhibition at 25 nM. With demonstrated anticancer activity in LoVo cells, ATR-IN-14 exhibits an IC50 of 64 nM. This reagent is valuable for researchers investigating DNA damage response mechanisms and therapeutic strategies in cancer treatment. -
ATR Inhibitor
ATR-IN-24 is a potent ATR (Ataxia Telangiectasia and Rad3-related protein) inhibitor. It exhibits significant anticancer activity by interfering with the DNA damage response pathway, thereby enhancing the effects of DNA-damaging agents. This compound is valuable for research applications targeting cancer cell proliferation and sensitivity to chemotherapy, making it an important tool for studies on tumor biology and treatment resistance. -
ATM Inhibitor
ATM Inhibitor-3 is a potent and selective inhibitor of the ataxia-telangiectasia mutated (ATM) kinase, demonstrating an IC50 of 0.71 nM. This compound specifically inhibits the PI3K kinase family, making it relevant for research in cancer biology and DNA damage response pathways. Additionally, ATM Inhibitor-3 exhibits favorable metabolic stability, making it a valuable tool for in vitro and in vivo studies. -
ATR Inhibitor
ATR-IN-6 is a selective inhibitor of ATR (ATM and Rad3-related), a serine/threonine kinase crucial for maintaining genomic stability and facilitating DNA damage repair, belonging to the phosphoinositide 3-kinase-related kinase (PIKK) family. This compound exhibits significant biological activity in the context of ATR-mediated pathways and holds promise for research in proliferative disorders and various cancer types. Its targeted inhibition of ATR can aid in the investigation of therapeutic strategies for diseases associated with DNA damage response dysfunction. -
ATR Inhibitor
ATR-IN-23 is a highly selective inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein) with an IC50 of 1.5 nM. This compound demonstrates significant antiproliferative activity against LoVo cancer cells and induces synthetic lethality in HT-29 cells. ATR-IN-23 is a valuable tool for investigating the mechanisms of DNA damage response (DDR) in cancer research, particularly in the context of DDR-deficient cancer types. -
ATM Inhibitor
ATM Inhibitor-4 is a potent and selective inhibitor of ATM (ataxia-telangiectasia mutated) kinase, exhibiting an IC50 of 0.32 nM. This compound demonstrates enhanced inhibition of the PI3K kinase family and achieves complete inhibition of mTOR at a concentration of 1 μM. Additionally, ATM Inhibitor-4 displays favorable metabolic stability, making it a valuable tool for research applications involving DNA damage response and cell cycle regulation. -
ATM Inhibitor
ATM Inhibitor-6 acts as a selective inhibitor of ATM kinase, interfering with the DNA damage response mechanism. It is valuable for studying cellular processes associated with DNA repair and the proliferation of cancer cells. This reagent is suitable for various cancer research applications, providing insights into the role of ATM in tumorigenesis and therapeutic resistance. -
ATM Inhibitor
ATM Inhibitor-11 is a potent ATM kinase inhibitor with an IC50 value of 0.32 nM. It effectively inhibits the phosphorylation of KAP1, demonstrating an IC50 of 0.97 nM. This compound shows significant pharmacokinetic properties, achieving high exposure levels in the brain, heart, and plasma of ICR mice. Additionally, ATM Inhibitor-11 displays notable anti-tumor activity in the NCI-H441 xenograft mouse model, making it a valuable tool for cancer research and therapeutic development. -
ATM/ATR Inhibitor
ATR-IN-10 is a selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase, exhibiting an IC50 value of 2.978 μM. This compound plays a crucial role in mediating the DNA damage response and is instrumental in studies related to cancer therapeutics, especially in enhancing the efficacy of DNA-damaging agents. ATR-IN-10 is particularly applicable in exploring the interplay between DNA repair mechanisms and cancer cell sensitivity, making it a valuable tool for research in oncology and molecular biology. -
ATR Inhibitor
ATR-IN-32 is a potent inhibitor of the ATR protein kinase, exhibiting oral bioavailability. This compound demonstrates a strong capacity to inhibit the proliferation of MIA PaCa-2 cells and effectively reduces tumor growth in mouse models bearing LOVO and HT-29 xenografts. ATR-IN-32 is applicable in the investigation of ATR-mediated cancer pathways, including those associated with colorectal and pancreatic cancers. -
ATR Inhibitor
ATR-IN-19 is a selective inhibitor of ATR (ATM and Rad3 related) kinase, functioning by disrupting the DNA damage response pathway. This compound has demonstrated potent biological activity in cellular models, making it an invaluable tool for studying the effects of ATR inhibition on cell cycle progression and DNA repair mechanisms. ATR-IN-19 can be employed in cancer research, particularly in investigating therapies that target DNA repair pathways in tumor cells. -
ATM Inhibitor
ATM-IN-1 is a specific inhibitor of Ataxia Telangiectasia Mutated (ATM) protein, which plays a crucial role in cell cycle regulation and the cellular response to DNA damage. By inhibiting ATM, this compound is instrumental in studying the mechanisms of cancer progression and neurological disorders. ATM-IN-1 is valuable for research applications focused on understanding the ATM signaling pathway and its implications in disease models.

