PI3K/Akt/mTOR

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  1. hAChE/hBuChE Inhibitor

    hAChE-IN-5 is a potent inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), exhibiting IC50 values of 0.17 μM for both enzymes. In addition, hAChE-IN-5 demonstrates significant GSK3β inhibition with an IC50 of 0.21 μM. This compound is utilized in research focused on tau protein aggregation and Aβ1-42 self-aggregation, effectively preventing Aβ-dependent neurotoxicity. Furthermore, hAChE-IN-5 can cross the blood-brain barrier, showcasing its potential as a multi-targeted agent in the study of Alzheimer's disease.
  2. GSK-3β inhibitor

    GSK-3β inhibitor 20 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 value of 74.4 nM. This compound is primarily utilized in research applications aimed at understanding the role of GSK-3β in various signaling pathways, including those involved in metabolism, neurodegenerative diseases, and cancer. Its effective inhibition can provide insights into GSK-3β functions and facilitate the development of therapeutic strategies targeting this kinase.
  3. GSK-3β Inhibitor

    18BIOder is a selective inhibitor of Glycogen Synthase Kinase 3 beta (GSK-3β) with notable neuroprotective properties. This compound has demonstrated efficacy in inhibiting HIV-1, contributing to its potential therapeutic applications in neurodegenerative diseases and HIV research. 18BIOder serves as a valuable tool for understanding the mechanistic pathways involved in GSK-3β modulation and its effects on cell signaling.
  4. GSK-3 Inhibitor

    GSK-3 Inhibitor 6 is a potent inhibitor of glycogen synthase kinase 3 (GSK-3), displaying IC50 values of 29 nM for GSK-3α and 24 nM for GSK-3β. This compound demonstrates effective central nervous system penetration, making it suitable for neurological research. It is beneficial for studying GSK-3-related pathways in various biological contexts, including cell signaling and neurodegenerative disease models.
  5. GSK-3β Inhibitor

    JGK-263 is an orally active inhibitor of Glycogen synthase kinase-3β (GSK-3β). It demonstrates neuroprotective properties and has the potential to enhance motor function. This compound is suitable for research applications related to neurological disorders, including amyotrophic lateral sclerosis (ALS).
  6. GSK-3 Inhibitor

    PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3), a key regulator in various cellular processes. This compound exhibits antioxidant and metal-chelating properties, contributing to its potential applications in neuroprotection. Research indicates that PIMPC may offer therapeutic benefits in conditions such as Alzheimer's disease, making it a valuable tool for studies focused on neurodegenerative disorders and GSK-3 modulation.
  7. CDK/GSK3 Inhibitor

    Aloisine RP106 is a potent inhibitor of cyclin-dependent kinases (CDKs) Cdk1/cyclin B and Cdk5/p25, as well as glycogen synthase kinase 3 (GSK3), with IC50 values of 0.70 µM, 1.5 µM, and 0.92 µM, respectively. This compound is valuable for research applications targeting cell cycle regulation and neurodegenerative diseases, where CDK and GSK3 activity contribute to pathological processes. Researchers can utilize Aloisine RP106 to investigate the role of these kinases in various biological contexts including cancer and neurobiology.
  8. PfGSK3/PfPK6 Inhibitor

    PfGSK3/PfPK6-IN-2 is a potent dual inhibitor of PfGSK3 and PfPK6, with IC50 values of 172 nM and 11 nM, respectively. This compound exhibits significant efficacy in the modulation of key signaling pathways in Plasmodium falciparum, making it a valuable tool for malaria research. Its ability to inhibit these targets can aid in the investigation of therapeutic strategies against malaria.
  9. GSK-3β Inhibitor

    GSK-3β Inhibitor 14 is a benzothiazepinone derivative that acts as a weak inhibitor of glycogen synthase kinase 3 beta (GSK-3β), with an IC50 greater than 100 μM. This compound is utilized in research focusing on GSK-3β-related pathways, potentially contributing to studies in various diseases, including neurodegenerative disorders and metabolic conditions. Its role in modulating GSK-3β activity makes it a valuable tool for elucidating the physiological and pathological functions associated with this important kinase.
  10. GSK-3β Inhibitor

    ZDWX-25 is a potent dual inhibitor of GSK-3β and DYRK1A, demonstrating an IC50 value of 71 nM for GSK-3β. This compound exhibits significant cytotoxic effects on SH-SY5Y and HL-7702 cell lines, making it a valuable tool for research in neurodegenerative diseases such as Alzheimer's disease. Its inhibitory action on key kinase pathways suggests potential for further exploration in therapeutic applications.
  11. GSK-3β/CDK-2/CDK-4 Inhibitor

    UNC10112785 is a potent inhibitor of serine/threonine kinases, specifically targeting GSK-3β, CDK-2, and CDK-4 with IC50 values of 0.031 μM, 0.016 μM, and 1.99 μM, respectively. This compound exhibits significant biological activity that positions it as a valuable tool in the study of type 2 diabetes. Its ability to modulate key pathways involved in metabolic regulation makes it an essential reagent for researchers investigating therapeutic interventions in diabetic conditions.
  12. GSK-3 Inhibitor

    BRD1652 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3), a critical regulator in various signaling pathways. This compound has shown potential in modulating GSK-3 activity, making it a valuable tool for investigating the molecular mechanisms underlying emotion-related disorders. Its application can enhance research on neuropsychiatric conditions and therapeutic strategies targeting GSK-3 signaling.
  13. GSK-3β Inhibitor

    Dihydronarwedine is an inhibitor of glycogen synthase kinase-3β (GSK-3β). At a concentration of 10 μM, it demonstrates a 39% reduction in GSK-3β activity. This compound is useful in research applications related to cellular signaling pathways, neurodegenerative diseases, and cancer therapy, where GSK-3β modulation is of interest.
  14. GSK-3 Inhibitor

    GSK-3 inhibitor 7 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3), a key regulator in various cellular processes. This compound demonstrates significant activity in modulating GSK-3 signaling pathways, making it a valuable tool for research in neurobiology and related fields. Its application may enhance understanding of GSK-3's role in neurodegenerative diseases and neuronal signaling.
  15. GSK-3 Inhibitor

    Cazpaullone is a potent glycogen synthase kinase-3 (GSK-3) inhibitor that plays a critical role in cellular signaling pathways. It enhances pancreatic beta cell protection and promotes their replication, making it valuable in diabetes research. Cazpaullone's mechanism of action provides insights into potential therapeutic strategies for diabetes and related metabolic disorders.
  16. GSK-3β Inhibitor

    GSK-3β inhibitor 25 primarily targets glycogen synthase kinase 3 beta (GSK-3β), demonstrating weak inhibitory activity with an IC50 greater than 100 μM. This compound is utilized in biochemical research to elucidate the role of GSK-3β in various signaling pathways and cellular processes, including metabolism and cell proliferation. Its modest potency may serve as a lead in the development of more selective GSK-3β inhibitors for therapeutic applications.
  17. GSK-3β Inhibitor

    GSK-3β inhibitor 26 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 18.23 μM. This compound is instrumental in research focusing on cancer, inflammation, and neurodegenerative diseases, facilitating the exploration of therapeutic pathways and mechanisms associated with GSK-3β modulation.
  18. GSK-3β Inhibitor

    TD114-2 is a potent and highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β), exhibiting an IC50 value of 48 nM. The compound forms a key hydrogen bond with arginine 141, which contributes to its remarkable specificity for GSK-3β compared to other kinases. TD114-2 is a valuable tool for investigating the role of GSK-3β in various conditions, including diabetes, neurodegenerative diseases, and other disorders linked to GSK-3β dysregulation.
  19. 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.
  20. 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.
  21. ATR Substrate

    ATR kinase substrate peptide (ASELPASQPQPFSAKKK) functions as a specific substrate for ATR protein kinase, facilitating the detection of ATR kinase activity in biological research. This peptide is instrumental in studying cellular responses to DNA damage and the associated signaling pathways. It plays a critical role in validating ATR kinase activity and exploring its implications in cancer biology and therapeutic development.
  22. 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.
  23. 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.
  24. PROTAC ATR Degrader

    PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies.
  25. 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.
  26. ATM/ATR

    SKLB-197 is a selective inhibitor of ATR (ATM and Rad3-related protein) with an IC50 value of 0.013 μM, demonstrating minimal activity against a panel of 402 other protein kinases. This compound exhibits significant antitumor efficacy specifically in ATM-deficient tumors, showing potent activity in both in vitro and in vivo models. SKLB-197 serves as a valuable tool for investigating the roles of ATM and ATR in cancer biology and for the development of targeted therapies.
  27. 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.
  28. 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.
  29. PROTAC ATR Degrader

    Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage.
  30. ATM Kinase Activity Inducer

    GJ071 oxalate is an ATM kinase activity inducer that targets ataxia telangiectasia mutated (ATM) kinase. It is specifically designed for use in A-T cells harboring homozygous TGA or TAG stop codons. This compound enhances ATM kinase activity, facilitating studies on DNA damage response mechanisms and therapeutic strategies for ataxia telangiectasia and related disorders.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. ATR Ligand

    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.
  40. 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.
  41. 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.
  42. ATR ligand

    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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. ATR Inhibitor

    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.
  48. ATR Inhibitor

    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.
  49. ATR Inhibitor

    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.
  50. ATR Inhibitor

    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.

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