PI3K/Akt/mTOR

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. ATM Inhibitor

    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.
  11. ATR Inhibitor

    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.
  12. ATR Inhibitor

    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.
  13. ATM Inhibitor

    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.
  14. ATM Inhibitor

    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.
  15. ATR Kinase Inhibitor

    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.
  16. ATR Inhibitor

    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.
  17. ATM Kinase Inhibitor

    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.
  18. ATR Inhibitor

    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.
  19. ATR Protein kinase Inhibitor

    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.
  20. ATR Inhibitor

    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.
  21. ATM/ATR Inhibitor

    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.
  22. ATM Inhibitor

    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.
  23. ATR Protein Kinase Inhibitor

    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.
  24. ATR Inhibitor

    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.
  25. ATR Inhibitor

    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.
  26. ATR Inhibitor

    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.
  27. DNA-PK/mTOR Inhibitor

    CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively disrupts signaling pathways associated with both mTORC1 and mTORC2. This compound is valuable for research focused on cancer therapeutics and the modulation of DNA damage response mechanisms.
  28. PI3K Inhibitor

    ETP-45658 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) family, exhibiting IC50 values of 22.0 nM for PI3Kα, 39.8 nM for PI3Kδ, 129.0 nM for PI3Kβ, and 717.3 nM for PI3Kγ. Additionally, ETP-45658 demonstrates inhibitory effects on DNA-PK (IC50 = 70.6 nM) and mTOR (IC50 = 152.0 nM). This compound is valuable for cancer research, particularly in exploring the roles of PI3K signaling pathways in tumorigenesis and treatment resistance.
  29. PI3Kδ Inhibitor

    PI3Kδ-IN-27 is a selective inhibitor of PI3Kδ, exhibiting an IC50 value of 355.3 nM. This compound demonstrates notable antiviral activity against SARS-CoV-2, making it a valuable tool for studying viral infections, particularly COVID-19. Researchers can utilize PI3Kδ-IN-27 to explore pathways related to immune response and infection mechanisms.
  30. PI4Kβ/PKG Inhibitor

    PI4Kβ/PKG-IN-2 is a potent dual inhibitor targeting Plasmodium phosphatidylinositol 4-kinase beta (PI4Kβ) and cGMP-dependent protein kinase (PKG). This compound demonstrates significant inhibitory activity against Plasmodium, making it a valuable tool for investigating malaria pathogenesis and potential therapeutic strategies. Its oral bioavailability further supports its use in preclinical studies aimed at understanding malaria biology.
  31. PfGSK3/PfPK6 Inhibitor

    PfGSK3/PfPK6-IN-1 is a selective inhibitor targeting PfGSK3 and PfPK6, with IC50 values of 97 nM and 8 nM, respectively. This compound effectively inhibits the proliferation of blood-stage Plasmodium falciparum 3D7 parasites, making it a valuable tool for malaria research. Additionally, PfGSK3/PfPK6-IN-1 exhibits low cytotoxicity in hepatocyte cultures at concentrations up to 200 nM, with a significant reduction in cell viability observed at 2 μM. Its dual action enhances its potential in studying malaria-related mechanisms and potential therapeutic strategies.
  32. Akt Inhibitor

    Miransertib mesylate is a potent and selective allosteric inhibitor of the Akt family, demonstrating IC50 values of 2.7 nM, 14 nM, and 8.1 nM for Akt1, Akt2, and Akt3, respectively. This compound is particularly effective against the AKT1-E17K mutant variant, making it valuable for investigating PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib mesylate has shown efficacy against Leishmania, highlighting its versatility in biological research applications.
  33. PI4KA Inhibitor

    PI4KA-IN-1 is a potent inhibitor of phosphatidylinositol 4-kinase alpha (PI4KA). This compound is valuable for studying the role of PI4KA in cellular processes and its implications in hepatitis C virus infection. By downregulating PI4KA activity, PI4KA-IN-1 can aid in elucidating the mechanisms of viral replication and pathogenesis, making it a useful tool for related therapeutic research and development.
  34. PI4KIIIα Inhibitor

    AZD2836 is a selective inhibitor of the host cell kinase PI4KIIIα. By targeting this kinase, AZD2836 disrupts the metabolism of phosphatidylinositol 4-phosphate (PI4P), a crucial component for the replication of hepatitis C virus (HCV). In studies using HCV subgenomic replicon cell lines, AZD2836 demonstrated effective antiviral activity, exhibiting EC50 values of 270 nM for genotype 1b (Con1 strain) and 550 nM for genotype 1a (Lemon strain). This compound serves as a valuable tool for researching viral replication mechanisms and assessing therapeutic options for HCV.
  35. MEK/PI3K Inhibitor

    MEK/PI3K-IN-2 is a potent inhibitor targeting both MEK and PI3K pathways, exhibiting IC50 values of 352 nM for MEK1, 107 nM for PI3Kα, and 137 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT and ERK1/2, demonstrating significant anti-proliferative activity against various tumor cell lines. MEK/PI3K-IN-2 is valuable for research in cancer biology and therapeutic development aimed at disrupting these critical signaling pathways.
  36. MEK/PI3K Inhibitor

    MEK/PI3K-IN-1 is a potent inhibitor targeting MEK and PI3K pathways, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT (pAKT) and ERK1/2 (pERK1/2), demonstrating significant anti-proliferative effects in various tumor cell lines. MEK/PI3K-IN-1 serves as a valuable tool for research in cancer therapeutics and signaling pathway analysis.
  37. Akt Kinase Inhibitor

    ML-9 Free Base is a selective and potent inhibitor of Akt kinase, demonstrating significant inhibitory effects on myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). It effectively inhibits MLCK, protein kinase A (PKA), and protein kinase C (PKC) with Ki values of 4 μM, 32 μM, and 54 μM, respectively. Additionally, ML-9 Free Base promotes autophagy by enhancing autophagosome formation while inhibiting their subsequent degradation, making it valuable for research on cellular signaling pathways and autophagic processes.
  38. AMPK Inhibitor

    BAY-3827 is a potent and selective inhibitor of AMP-activated protein kinase (AMPK), exhibiting IC50 values of 1.4 nM at low ATP concentrations (10 μM) and 15 nM at higher ATP concentrations (2 mM). This compound demonstrates over 500-fold selectivity against a wide array of kinases, making it a valuable tool for elucidating AMPK-related pathways. BAY-3827 effectively inhibits the phosphorylation of acetyl-CoA carboxylase 1 and displays significant anti-proliferative effects in androgen-dependent prostate cancer cell lines, supporting its application in cancer research and metabolic studies.
  39. AMPK Inhibitor

    AMPK-IN-3 is a potent and selective inhibitor of AMP-activated protein kinase (AMPK), exhibiting IC50 values of 60.7 nM for AMPK α2, 107 nM for AMPK α1, and 3820 nM for KDR. This compound effectively inhibits AMPK without impacting cell viability or inducing significant cytotoxicity in K562 cells. AMPK-IN-3 is valuable for research focused on cancer biology and the role of AMPK in metabolic regulation and cellular energy homeostasis.
  40. AMPK Inhibitor

    Chromium(III) acetate functions as an AMPK inhibitor by inhibiting the phosphorylation of AMP-activated protein kinase (AMPK), subsequently promoting lipogenesis. This compound exhibits low toxicity in mammalian models, demonstrated by an LD50 of 2365 mg/kg in rats. It is primarily utilized in research to explore metabolic pathways and the regulation of energy homeostasis.
  41. AMPK Inhibitor

    AMPK-IN-4 is a selective inhibitor of AMP-activated protein kinase (AMPK), targeting both AMPKα1 and AMPKα2 with IC50 values of 393 nM and 141 nM, respectively. This compound is significant in cancer research, facilitating investigations into metabolic regulation and cellular energy homeostasis. Its efficacy in modulating AMPK activity makes it a valuable tool for studying the pathways associated with tumor metabolism and potential therapeutic strategies.
  42. mTOR Inhibitor/AMPK Activator

    AMPK/mTOR modulator-1 is a Ginsenoside derivative functioning as both an mTOR inhibitor and AMPK activator. It activates AMPK signaling with a Kd of 4.759 μM, promoting M1-like tumor-associated macrophage polarization while inhibiting M2-like polarization. This compound enhances glycolysis and demonstrates significant anti-inflammatory activity alongside inhibition of tumor progression. AMPK/mTOR modulator-1 is ideal for research focused on colorectal cancer and related metabolic disorders.
  43. PI4K Inhibitor

    KAI-407 is an orally active inhibitor targeting Plasmodium PI4K kinase, effectively disrupting multiple stages of the parasite lifecycle. It demonstrates EC50 values of 81 nM against the blood stages of malignant Plasmodium and 88 nM for liver schizonts of P. yoelii. Additionally, KAI-407 exhibits IC50 values of 0.64 μM and 0.69 μM for liver schizonts and dormant bodies of P. cynomolgi, respectively. This compound is valuable for investigating vivax malaria and assessing potential therapeutic strategies against Plasmodium berghei infections.
  44. PI4K Inhibitor

    BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ), exhibiting an IC50 of 5.7 nM. This compound effectively modulates lipid metabolism and signaling pathways involved in cellular processes. BF738735 is leveraged in research to investigate PI4KIIIβ's role in various diseases, including cancer and viral infections, highlighting its potential for therapeutic development.
  45. PI4KB Inhibitor

    PI4K-IN-2 is a highly selective inhibitor of phosphatidylinositol 4-kinase β (PI4KB) with an IC50 of 0.015 μM. This compound demonstrates significant inhibitory activity and is particularly relevant for research involving human rhinovirus (HRV). Its potential applications extend to studies focusing on the role of PI4KB in viral replication and related signaling pathways.
  46. PI4KIIIα Inhibitor

    GSK-A1 is a selective inhibitor of type III phosphatidylinositol 4-kinase PI4KIIIα, exhibiting a pIC50 of 8.5-9.8. It effectively inhibits the resynthesis of PtdIns(4,5)P2 with an IC50 of approximately 3 nM, leading to a potent decrease in PtdIns(4)P levels without significantly affecting PtdIns(4,5)P2. GSK-A1 serves as a valuable tool in research aimed at understanding its potential role in anti-hepatitis C virus (HCV) applications.
  47. PI4KIIIβ Inhibitor

    MI 14 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ), demonstrating an IC50 of 54 nM for this target, while exhibiting limited activity against PI4KIIIα and PI4KIIα with IC50s greater than 100 μM. This compound displays notable antiviral efficacy against hepatitis C virus (HCV) genotype 1b, Coxsackievirus B3 (CVB3), human rhinovirus (HRV), and HCV genotype 2a. MI 14 serves as a valuable tool for research focused on viral pathogenesis and therapeutic interventions targeting lipid kinase signaling pathways.
  48. PI4KIIIα/HCV Inhibitor

    AL-9 is a potent inhibitor of phosphatidylinositol 4-kinase III alpha (PI4KIIIα) with an IC50 of 0.57 μM. It effectively disrupts hepatitis C virus (HCV) replication, making it a valuable tool for studying viral pathogenesis and potential antiviral strategies. Its selective targeting of PI4KIIIα highlights its relevance in research applications focused on HCV infection and related therapeutic developments.
  49. mTOR Inhibitor

    Aschantin is a bisepoxylignan that acts as a potent mTOR kinase inhibitor. This compound demonstrates significant biological activities, including antiplasmodial effects, calcium channel antagonism, and the inhibition of platelet activating factor. Additionally, Aschantin serves as an inhibitor of Cytochrome P450 and UGT enzymes, making it a valuable tool for chemoprevention research and various biochemical studies.
  50. mTORC1 Inhibitor

    Sulindac sulfone is an mTORC1 pathway inhibitor and an active metabolite of Sulindac. It has been shown to effectively inhibit the growth of colon cancer cells and induce cell cycle arrest, making it a valuable tool in cancer research. This compound is primarily utilized to study the role of mTORC1 in tumorigenesis and to explore potential therapeutic strategies against colorectal cancer.

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