PI3K/Akt/mTOR

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. PI3K Inhibitor

    AS-605240 is an orally active inhibitor of PI3-kinase γ that inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.
  17. AKT inhibitor

    AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A.
  18. mTOR Inhibitor

    Deforolimus (Ridaforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.

  19. PI3K Inhibitor

    IC-87114 was the first isoform-selective PI3K inhibitor :p110M-NM-4(IC50 = 0.13 M-BM-5M) vs. p110M-NM-1(IC50 = 200 M-BM-5M), p110M-NM-2(IC50 = 16 M-BM-5M) and p110M-NM-3(IC50 = 61 M-BM-5M).
  20. CDK & GSK-3β inhibitor

    Indirubin, the active constituent of a Chinese antileukaemia medicine, is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.
  21. mTOR Inhibitor

    KU-0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2 respectively).
  22. AKT Inhibitor

    Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation.
  23. PI3K inhibitor

    PIK-293 is a PI3-K inhibitor. PIK-293 inhibits the p110α, p110β, p110δ. PIK-293 is the parent compound of PIK-294.
  24. PI3K inhibitor

    PIK-294 is a PI3 Kinase inhibitor that is 20- to 60-fold more potent than the parent compound, PIK-293. It is one of the most potent p110δ-selective inhibitors that has been reported.
  25. PI3K Inhibitor

    PIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity.
  26. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  27. GSK-3 inhibitor

    SB 216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).
  28. PI3K/mTOR inhibitor

    Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
  29. mTOR inhibitor

    Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells.
  30. PI3K Inhibitor

    TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).
  31. PI3K inhibitor

    XL765 is a PI3K/mTOR dual kinase inhibitor and it is more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.
  32. AKT Inhibitor

    CCT128930 is an ATP-competitive AKT inhibitor that is a potent, advanced lead pyrrolopyrimidine compound exhibiting selectivity for AKT over PKA, achieved by targeting a single amino acid difference.
  33. AKT Inhibitor

    PHT-427 is a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.
  34. AKT Inhibitor

    Triciribine phosphate inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation.
  35. mTOR/PI3K Inhibitor,

    GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
  36. mTOR Inhibitor

    WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks).
  37. mTOR inhibitor

    OSI-027 is a potent, selective and orally bioavailable mTOR kinase inhibitor that inhibits the kinase activity associated with both the TORC1 and TORC2 complexes of mTOR.
  38. GSK-3 inhibitor

    SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM.
  39. GSK-3 inhibitor

    CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3.
  40. ATM inhibitor

    CP-466722 is a specific ATM inhibitor that inhibits cellular ATM-dependent phosphorylation events and disruption of ATM function resulted in characteristic cell cycle checkpoint defects.
  41. PI3K inhibitor

    PKI-402 is a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.
  42. PI3K inhibitor

    AS-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000, and 20,000 nM respectively.
  43. ATR inhibitor

    Camonsertib is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. 

  44. GSK3α inhibitor

    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor.
  45. PI3Kβ inhibitor

    AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm).
  46. PI3K inhibitor

    MDK34597 is a PI3K inhibitor. MDK34597 has CAS#371934-59-7, the last 5 digits of which were used for its name. MDK34597 is an analog of PI-103 and acts as a dual PI3K/mTOR Inhibitor.
  47. ILK inhibitor

    ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
  48. PI3Kα Inhibitor

    Tersolisib is a selective allosteric inhibitor of PI3Kα, specifically designed to target mutant forms of the enzyme. This compound exhibits significant anti-tumor activity, demonstrating robust and durable regression in various cancer models. Tersolisib is valuable in cancer research, particularly for studies focusing on PI3K pathway alterations and their therapeutic implications.
  49. PI3K/Akt/mTOR Inhibitor

    Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy.
  50. PI3Kα Inhibitor

    BBO-10203 is a potent PI3Kα inhibitor that selectively and covalently binds to Cys242 in the RAS-Binding Domain. It inhibits both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. By disrupting the interaction between RAS isoforms and PI3Kα, BBO-10203 effectively reduces pERK expression, suppresses cell growth, and induces G1 arrest and apoptosis. This compound is valuable for research into breast cancer, colorectal cancer, and non-small cell lung cancer.

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