ATM/ATR

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-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-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.

ATR-IN-30 is a selective ATR (ataxia telangiectasia and Rad3-related protein) ligand that plays a crucial role in disrupting ATR signaling pathways. This compound can be utilized for the development of ATR PROTACs, including PROTAC ATR degrader-2, facilitating targeted protein degradation studies. ATR-IN-30 is valuable for researchers investigating DNA damage response mechanisms and potential therapeutic avenues in cancer treatment.

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-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.

ATR Ligand 2 targets the ATR protein as a PROTAC ligand, facilitating the degradation of ATR through the ubiquitin-proteasome system. By conjugating ATR Ligand 2 with an E3 ligase ligand and linker, researchers can synthesize PROTAC ATR degrader-3, enabling the selective modulation of ATR levels in cells. This compound is instrumental for studies focusing on DNA damage response, cancer therapeutics, and the mechanism of action of DNA-targeting agents.

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-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-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-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.

ATR-IN-15 is a potent inhibitor of ATR kinase, exhibiting an IC50 of 8 nM. This compound demonstrates significant inhibitory effects on human colon tumor cells (LoVo) as well as DNA-PK and PI3K, with IC50 values of 47 nM, 663 nM, and 5131 nM, respectively. ATR-IN-15 is valuable for research into DNA damage response pathways and cancer therapeutics.

ATR-IN-21 is a potent inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR), exhibiting an IC50 value of less than 1000 nM. This compound effectively modulates the DNA damage response, making it valuable for research in cancer biology and therapeutic development. ATR-IN-21 can be utilized in studies exploring tumor cell sensitivity to genotoxic agents and the mechanistic pathways of DNA repair.

ATR-IN-17 is a potent inhibitor of the Ataxia Telangiectasia and Rad3 related (ATR) kinase. Demonstrating significant anticancer activity, ATR-IN-17 exhibits an IC50 value of 1 nM in LoVo cells, making it a valuable tool for cancer research. This compound is primarily utilized in studies focusing on DNA damage response and cell cycle regulation.

ATR-IN-22 is a potent inhibitor of Ataxia Telangiectasia and Rad3-related protein (ATR). This compound effectively reduces the proliferation of MIAPaCa-2 pancreatic cancer cells, exhibiting an IC50 of less than 1 μM. Additionally, ATR-IN-22 demonstrates significant anti-tumor activity in colon cancer, making it a valuable reagent for research into cancer biology and therapeutic development.

ATM Inhibitor-2 is a highly potent and selective inhibitor of ataxia telangiectasia mutated (ATM) kinase, exhibiting an IC50 of less than 1 nM. This compound is valuable in studying DNA damage response mechanisms and cell cycle regulation. Researchers can utilize this inhibitor to explore potential therapeutic strategies in cancer treatments and related biological pathways.

ATR-IN-20 is a potent inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein) with an IC50 value of 3 nM. In addition to its primary action on ATR, ATR-IN-20 also inhibits mTOR with an IC50 of 18 nM while demonstrating selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). This compound shows a favorable pharmacokinetic profile with 30% oral bioavailability, indicating its potential for applications in anticancer research and therapeutic development.

ATR-IN-8 is a potent inhibitor of ATR (ataxia telangiectasia and Rad3-related protein), a critical enzyme involved in the homologous recombination repair pathway and a member of the PIKK family. This compound demonstrates significant biological activity in disrupting ATR-mediated DNA damage response mechanisms, making it a valuable tool for cancer research. ATR-IN-8 can be utilized to investigate the therapeutic implications of ATR inhibition in various cancer models and studies related to DNA repair mechanisms.

Antitumor agent-28 is a selective inhibitor of ataxia telangiectasia mutated (ATM) kinase. By inhibiting ATM activity, it disrupts DNA damage response pathways, demonstrating potent anti-cancer efficacy. This compound is valuable for research applications focused on cancer biology, DNA repair mechanisms, and therapeutic development.

ATM-IN-12 is a specific inhibitor of ATM kinase, exhibiting an IC50 of 1.26 μM. This compound is instrumental in studying ATM kinase-mediated diseases, particularly in cancer research. By targeting ATM kinase, ATM-IN-12 provides valuable insights into the cellular responses to DNA damage and the mechanisms underlying tumorigenesis.

ATR-IN-29 is a highly potent ATR kinase inhibitor, demonstrating an IC50 value of 1 nM. This compound exhibits significant antiproliferative activity, making it a valuable tool for investigating the role of ATR in cancer cell proliferation. ATR-IN-29 is ideal for studies focused on DNA damage response and cell cycle regulation, providing insights into therapeutic interventions for cancer treatment.

ATR-IN-13 is a potent inhibitor of ATR kinase, exhibiting an IC50 of 2 nM. This compound is primarily utilized in research related to ATR kinase-mediated diseases, including proliferative disorders and various forms of cancer. Its specific inhibitory activity makes it a valuable tool for exploring the roles of ATR kinase in tumor biology and therapeutic interventions.

ATM-IN-13 is a selective inhibitor of ATM kinase, exhibiting an IC50 of 0.3 nM in human cells. This compound effectively disrupts the ATM-mediated signaling pathway responsible for DNA double-strand break repair, resulting in decreased phosphorylation of ATM and p53 and inhibiting the ATM-dependent DNA damage response. ATM-IN-13 is a valuable tool for advancing research in colorectal cancer and understanding the mechanisms of DNA repair and cellular response to genotoxic stress.

ATR-IN-18 is a potent and orally active ATR kinase inhibitor with an IC50 of 0.69 nM. It exhibits significant antiproliferative effects in LoVo cells, achieving an IC50 of 37.34 nM. Due to its inhibitory effects on ATR, ATR-IN-18 is relevant for research applications in cancer biology and therapeutic development.

ATR kinase-IN-2 is a selective inhibitor of ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM. This compound is valuable for investigating the role of ATR in DNA damage response pathways and its implications in cancer biology. Research applications include exploring tumor cell sensitivity to DNA-damaging agents and elucidating mechanisms of resistance to cancer therapies.

ATR-IN-5 is a potent inhibitor of ATR (Ataxia Telangiectasia and Rad3-related protein), a member of the PI3K-related kinase family that plays a crucial role in maintaining genome stability and facilitating DNA damage repair. This compound is valuable for research into ATR kinase-mediated diseases, including various proliferative disorders and cancers. Its inhibitory effects on ATR provide a useful tool for investigating therapeutic strategies targeting DNA repair mechanisms in these conditions.

ATM Inhibitor-9 is a selective inhibitor targeting ATM kinase, with an IC50 value of 5 nM. It effectively impairs ATM-mediated signaling pathways, making it an invaluable tool for cancer research, particularly in studies involving DNA damage response and repair mechanisms. This compound can be used to explore the role of ATM in tumor biology and therapeutic resistance.

ATM Inhibitor-8 is a selective and potent inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 1.15 nM. This compound demonstrates significant anti-tumor activity, making it valuable for research in cancer biology and therapeutic development. Its oral bioavailability enhances its utility in in vivo studies exploring the role of ATM inhibition in various malignancies.

ATR kinase-IN-3 is a potent ATR protein kinase inhibitor with a Ki value ranging from 0.01 to 1 μM. This compound significantly modulates the ATR signaling pathway, making it valuable for studies in cancer biology, particularly in understanding DNA damage response mechanisms. Its ability to inhibit ATR activity can aid in assessing the therapeutic potential of targeting this pathway in various cancer models.

ATR-IN-16 is a potent inhibitor of the ATR kinase, a critical regulator of the DNA damage response pathway. This compound demonstrates significant anticancer activity, exhibiting an IC50 of 410 nM in LoVo cells. ATR-IN-16 is applicable in cancer research, particularly for studies focused on DNA repair mechanisms and therapeutic strategies targeting ATR signaling.

ATR-IN-33 is a selective ATR kinase inhibitor that targets the ataxia telangiectasia and Rad3-related protein, involved in the DNA damage response. By inhibiting ATR activity, ATR-IN-33 effectively impairs cellular repair mechanisms, which can lead to enhanced sensitivity to DNA-damaging agents. This compound is valuable for research applications in cancer biology, particularly in studies assessing tumor response to therapy and exploring mechanisms of resistance.

Ceralasertib formate is a highly potent and selective inhibitor of ATR (ataxia telangiectasia and Rad3-related protein) with an IC50 value of 1 nM. This compound effectively inhibits cell viability, induces DNA damage, and promotes cellular senescence. Ceralasertib formate demonstrates notable antitumor activity and is valuable for research applications focused on cancer therapeutics and DNA damage response pathways.