PI3K/Akt/mTOR

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  1. COX-2/PI3K Inhibitor

    COX-2/PI3K-IN-2 is a potent inhibitor targeting both COX-2 and PI3K pathways, exhibiting an IC50 value of 2.78 nM for PI3K and a Ki value of 3.02 nM for COX-2. This compound demonstrates significant anti-inflammatory and anti-cancer activities, making it valuable for research in oncology and inflammatory disease studies. Its dual-target mechanism provides insights into the therapeutic potential of modulating these critical pathways.
  2. PI3Kα Inhibitor

    VVD-442 is a selective inhibitor of PI3Kα that covalently binds to cysteine 242 within the RAS-binding domain of the PI3K p110α subunit. This binding induces conformational changes that disrupt the interaction between PI3K p110α and RAS proteins, effectively blocking RAS-mediated activation of PI3K. VVD-442 is applicable in research focusing on RAS-mutant cancers and HER2-overexpressing tumors, providing valuable insights into therapeutic strategies targeting these pathways.
  3. PI3Kδ Inhibitor

    LAS195319 is a potent and orally active inhibitor of PI3Kδ, exhibiting an IC50 of 0.5 nM. This compound demonstrates high selectivity against a wide array of proteins, lipid kinases, and GPCRs. LAS195319 effectively inhibits the infiltration of neutrophils and eosinophils, making it a valuable tool for research into respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD).
  4. 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.
  5. 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.
  6. Nrf2/AMPK/mTOR Activator

    Hydroxycitric acid is an orally active compound that serves as a multifunctional activator of Nrf2, AMPK, and mTOR pathways. It enhances the expression of antioxidant enzymes, such as superoxide dismutase, and increases glutathione levels, thereby mitigating oxidative stress and ferroptosis, particularly in renal tubular epithelial cells. Additionally, hydroxycitric acid induces cell cycle arrest in cancer cells and promotes DNA fragmentation through modulation of the AMPK and mTORC1/S6K signaling pathways. This compound is valuable for research in oxidative stress, cancer biology, and metabolic regulation.
  7. PI3Kδ Inhibitor

    IHMT-PI3Kδ-372 is a highly selective inhibitor of PI3Kδ, exhibiting an IC50 of 14 nM. This compound demonstrates significant selectivity over other class I PI3Ks, with 56 to 83-fold differences, as well as over various protein kinases. IHMT-PI3Kδ-372 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), enabling investigations into therapeutic strategies targeting this pathway.
  8. PI3K Inhibitor

    Isopsoralidin is a phosphatidylinositol 3-kinase (PI3K) inhibitor that demonstrates potentially hepatotoxic properties and exhibits inhibitory activity on CYP2D6. This compound plays a significant role in research focused on cell signaling pathways related to cancer and metabolic disorders. Its unique mechanism of action makes it a valuable tool for studying PI3K-related biological processes and evaluating therapeutic approaches involving PI3K modulation.
  9. mTORC1/glucose transporter Inhibitor

    NV-5440 is an inhibitor of the mechanistic target of rapamycin complex 1 (mTORC1) and glucose transporters GLUT-1, GLUT-2, GLUT-3, and GLUT-4. This compound effectively inhibits glucose uptake in cells, providing valuable insights into glucose metabolism and its regulation. NV-5440 is useful for research applications involving cancer metabolism, diabetes, and other metabolic disorders where mTORC1 signaling and glucose transport play significant roles.
  10. mTORC1/S6K1 Inhibitor

    Coronarin A is a natural compound that functions as an inhibitor of mTORC1 and S6K1, enhancing IRS1 activity. This compound exhibits anti-inflammatory properties and is relevant for research into type 2 diabetes mellitus. Its modulation of key signaling pathways makes Coronarin A a valuable tool for studying metabolic disorders and inflammation-related conditions.
  11. mTOR

    Dioctanoylphosphatidic acid sodium acts as a modulator of the mammalian target of rapamycin (mTOR) signaling pathway. This compound enhances phagocyte respiratory burst, serves as a precursor for diacylglycerol and lysophosphatidic acid, and improves the viability of gallbladder carcinoma cells when used in conjunction with histone deacetylase inhibitors (HDACIs). Its unique biosynthetic origins from glycerophospholipid highlight its relevance in cellular signaling research and cancer studies.
  12. AMPK/SIRT3/PGC-1α Modulator

    MitoPBN is an AMPK/SIRT3/PGC-1α modulator that enhances mitochondrial function by acting as a reactive oxygen species scavenger. This compound promotes mitochondrial biogenesis through increased AMPK phosphorylation, restoration of SIRT3 expression, and upregulation of PGC-1α. MitoPBN is effective in regulating glucose metabolism, as it decreases blood glucose levels by inhibiting hepatic gluconeogenesis and enhancing glucose uptake, while also improving ATP production and maintaining mitochondrial membrane potential. Additionally, it can reduce apoptosis and enhance sperm motility and membrane integrity, making it a valuable reagent for research related to diabetes and metabolic disorders.
  13. PI3K Kinase Ligand

    HL-2 is a selective ligand for the phosphoinositide 3-kinase (PI3K) kinase, utilized in the synthesis of proteolysis-targeting chimeras (PROTACs). Its role in modulating PI3K activity makes it a valuable tool for studying signal transduction pathways and cancer biology. HL-2's application extends to drug development and the investigation of therapeutic strategies targeting PI3K-related diseases.
  14. PI3K/mTOR Inhibitor

    DS-7423 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 15.6 nM for PI3Kα and 34.9 nM for mTOR. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer biology and potential therapeutic strategies. Its ability to inhibit key signaling pathways involved in cell growth and survival positions DS-7423 as a promising candidate for further exploration in oncology studies.
  15. PI3K/mTOR Inhibitor

    PI3K-IN-37 is a potent inhibitor of the PI3K family, specifically targeting PI3K α, β, and δ isoforms with IC50 values of 6, 8, and 4 nM, respectively. Additionally, PI3K-IN-37 demonstrates strong inhibition of mTOR with an IC50 of 4 nM. This compound is valuable for research applications involving cancer biology, metabolic disorders, and signaling pathways related to cell growth and survival.
  16. PI3Kα/mTOR Kinase Inhibitor

    PI3K-IN-22 is a potent dual inhibitor of the PI3Kα and mTOR kinases, with IC50 values of 0.9 nM and 0.6 nM, respectively. This compound exhibits substantial biological activity, making it valuable for investigating the roles of these pathways in cancer research. PI3K-IN-22 can facilitate the study of tumor growth and response to therapy, contributing to the understanding of oncogenic signaling and potential treatment strategies.
  17. Dual PI3K/mTOR Inhibitor

    PKI-179 hydrochloride is a potent dual inhibitor of the PI3K and mTOR signaling pathways, demonstrating IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. This compound is effective against mutant variants E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride has been shown to exhibit significant anti-tumor activity in vivo, making it a valuable tool for cancer research and therapeutic development targeting PI3K/mTOR pathways.
  18. PI3K/mTOR Inhibitor

    SN32976 is a potent and selective inhibitor of class I phosphoinositide 3-kinases (PI3K) and mTOR, exhibiting IC50 values of 15.1 nM for PI3Kα, 461 nM for PI3Kβ, 110 nM for PI3Kγ, 134 nM for PI3Kδ, and 194 nM for mTOR. This compound demonstrates significant selectivity against a wide panel of 442 kinases. SN32976 is primarily utilized in cancer research, showcasing notable anticancer activity that makes it a valuable tool for studying PI3K/mTOR pathway modulation.
  19. mTOR Inhibitor

    MHY-1685 is a novel inhibitor of the mammalian target of rapamycin (mTOR), a key regulator of cell growth and metabolism. This compound demonstrates significant potential in promoting human cardiac stem cell (hCSC)-based myocardial regeneration. Its efficacy in modulating the mTOR pathway makes MHY-1685 a valuable tool for researchers investigating cardiac repair mechanisms and therapies.
  20. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-13 sodium is a dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and mTOR kinase, demonstrating oral bioavailability. This compound exhibits significant biological activity in the modulation of cellular growth and metabolism, making it a valuable tool in research related to sexual dysfunction, solid tumors, and idiopathic pulmonary fibrosis (IPF). Its dual inhibition profile presents opportunities for therapeutic exploration in various disease contexts.
  21. PI3K/mTOR inhibitor

    PI3K-IN-18 is a potent inhibitor of the PI3K/mTOR signaling pathway, selectively targeting PI3K-α and mTOR with IC50 values of 41 nM and 49 nM, respectively. This compound exhibits significant biological activity by disrupting key signaling processes involved in cell growth and proliferation. PI3K-IN-18 is valuable for research applications focused on cancer biology, metabolism, and therapeutic strategies targeting the PI3K/mTOR axis.
  22. mTORC1/2 Inhibitor

    Dihydroevocarpine is a selective inhibitor of mTORC1 and mTORC2, exhibiting potent cytotoxic effects in acute myeloid leukemia cells. By effectively suppressing mTORC1/2 activity, it disrupts critical signaling pathways involved in cell proliferation and survival. This compound is valuable for research focused on cancer biology and the development of targeted therapies for hematological malignancies.
  23. PI3K Inhibitor

    PI3Kα/mTOR-IN-1 is a selective dual inhibitor targeting PI3Kα and mTOR, exhibiting an IC50 of 7 nM for PI3Kα in cellular assays. It demonstrates Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in cell-free assays, respectively. This compound is instrumental in studies related to cancer biology and signal transduction, making it valuable for research involving the modulation of PI3K/mTOR pathways.
  24. mTORC Inhibitor

    OXA-01 is a potent inhibitor of the mammalian target of rapamycin complex 1 (mTORC1) and complex 2 (mTORC2), exhibiting IC50 values of 29 nM and 7 nM, respectively. This compound effectively disrupts mTOR signaling, which plays a crucial role in cellular growth, metabolism, and proliferation. OXA-01 is valuable for research applications investigating cancer, metabolic disorders, and the modulation of cellular signaling pathways.
  25. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-9 is a potent inhibitor targeting both the PI3K and mTOR pathways, exhibiting IC50 values of 38 nM for mTOR (in phospho-S6 cellular assays) and 6.6 μM, 6.6 μM, and 0.8 μM for PI3Kα, PI3Kγ, and PI3Kδ, respectively. This compound demonstrates significant biological activity in modulating cellular growth and metabolism, making it a valuable tool for research on cancer and other diseases characterized by dysregulated PI3K/mTOR signaling. Its application in various cellular models facilitates the exploration of therapeutic strategies in oncology and other fields of biomedical research.
  26. mTOR Inhibitor

    mTOR inhibitor-23 (compound DHM25) is a selective and irreversible covalent inhibitor of the mechanistic target of rapamycin (mTOR). It functions through covalent interaction with a nucleophilic amino acid in the ATP binding pocket, effectively modulating mTOR signaling pathways. This compound demonstrates significant antitumor activity against triple-negative breast cancer cell lines, highlighting its potential in cancer research and therapeutic applications.
  27. mTOR Inhibitor

    AV457 is a potent and selective inhibitor of the mTOR pathway, exhibiting an IC50 value of 0.54 µM. This compound has demonstrated efficacy in reducing cyst growth in organoids derived from polycystic kidney disease (PKD). Additionally, AV457 effectively lowers the protein expression levels of P-S6 and P-P70S6, while leaving P-AKT levels unchanged, making it a valuable tool for investigating mTOR-related signaling in various biological contexts.
  28. mTOR Inhibitor

    mTOR inhibitor-12 is a selective inhibitor of the mechanistic target of rapamycin (mTOR) that effectively penetrates the blood-brain barrier. This compound demonstrates significant potential in modulating mTOR signaling pathways, making it valuable in the study of central nervous system (CNS) disorders. Additionally, mTOR inhibitor-12 has been assessed for its non-genotoxic properties, facilitating safer applications in neurological research.
  29. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-5 selectively targets both phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), demonstrating IC50 values of 86.9 nM for PI3K and 14.6 nM for mTOR. This dual inhibition has significant implications for cancer research, as it can effectively impede cell proliferation and survival in tumor cells. PI3K/mTOR Inhibitor-5 is suitable for studies investigating the PI3K/mTOR signaling pathway and its role in various diseases, particularly in the contexts of oncology and metabolic disorders.
  30. mTOR Inhibitor

    PF-05139962 is a cyclic sulfone compound that acts as a potent inhibitor of the mTOR kinase. It demonstrates strong inhibitory activity with a Ki of 5 nM and IC50 values of 48 nM for phosphorylated S473 and 6 nM for phosphorylated S6, highlighting its high selectivity. This compound is valuable for research applications involving cell growth, metabolism, and cancer therapy, particularly in studies focused on mTOR signaling pathways.
  31. mTOR Inhibitor

    RMC-4529 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), demonstrating an IC50 value of 1.0 nM against phosphorylated 4E-BP1 at threonine 37/46 in cellular assays. This compound is valuable for research applications focused on mTOR signaling pathways, potentially impacting studies in cancer, metabolism, and neurodegenerative diseases. Its selectivity and efficacy make it a useful tool for investigating the role of mTOR in various biological processes.
  32. mTOR Inhibitor

    GNE-555 is a selective, metabolically stable inhibitor of the mechanistic target of rapamycin (mTOR), with a Ki value of 1.5 nM. This compound demonstrates significant antiproliferative effects on prostate cancer (PC3) and breast cancer (MCF-7) cell lines. GNE-555 is ideal for applications in cancer research, particularly in studies exploring mTOR signaling pathways and their role in tumorigenesis.
  33. mTOR Inhibitor

    eCF309 is a potent and selective mTOR inhibitor, exhibiting an IC50 of 15 nM. This compound demonstrates heightened selectivity over PI3 kinases, making it a valuable tool for research. eCF309 is particularly relevant in the study of breast cancer and prostate cancer, facilitating investigations into the mechanistic roles of mTOR signaling in these diseases.
  34. mTOR Degrader

    PD-M6 is an mTOR-targeted PROTAC degrader that facilitates the ubiquitination and subsequent degradation of mTOR, exhibiting a DC50 of 4.8 μM. This compound has demonstrated potent anti-proliferative effects on HeLa, MCF-7, and HepG2 cancer cell lines, with IC50 values of 11.3, 2.58, and 3.23 μM, respectively. Additionally, PD-M6 induces autophagy and specifically promotes the degradation of LAMTOR1, a pivotal component of the mTOR signaling pathway, suggesting its utility for investigating mTOR-related biological processes in cancer research.
  35. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-3 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and mechanistic target of rapamycin (mTOR). This imidazoline derivative exhibits significant anti-cancer activity, making it a valuable tool for cancer research. Its ability to modulate key signaling pathways related to cell growth and survival enhances its utility in studying tumor biology and therapeutic strategies.
  36. PI3Kα/mTOR Inhibitor

    PI3Kα-IN-5 is a potent inhibitor of the PI3Kα and mTOR pathways, exhibiting IC50 values of 0.7 nM and 3.3 nM, respectively. This compound is valuable for research focused on colorectal cancer, offering insights into the modulation of these critical signaling pathways. Its specificity and efficacy make it an important tool for investigating the roles of PI3Kα and mTOR in cancer biology.
  37. mTOR Inhibitor

    mTOR Inhibitor-11 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 21 nM for phosphorylated S6 ribosomal protein. This compound also demonstrates inhibitory activity against checkpoint kinase 1 (pCHK1) and phosphodiesterase 4D (PDE4D), with IC50 values of 17.2 μM and 17.0 μM, respectively. mTOR Inhibitor-11 is suitable for research on central nervous system (CNS) diseases, facilitating studies into neurodegenerative conditions and other related disorders.
  38. mTOR Inhibitor

    PP30 is a potent, selective ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 80 nM. This compound demonstrates significant inhibition of mTOR signaling, making it valuable for research focused on cell growth, proliferation, and survival pathways. PP30 is applicable in studies related to cancer, metabolic disorders, and various diseases involving dysregulation of mTOR pathways.
  39. mTORC1 Pathway Inhibitor

    CIDD 0067106 is a selective inhibitor of the mTORC1 pathway, specifically designed for targeting androgen receptor-positive (AR+) triple-negative breast cancer (TNBC). It exhibits potent activity against AR+ TNBC cell lines, with a GI50 value of 0.8 μM, indicating its effectiveness in inhibiting cancer cell proliferation. This compound is valuable for research focused on understanding and developing treatments for AR+ TNBC.
  40. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-12 is a selective inhibitor targeting the phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways, exhibiting IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Additionally, PI3K/mTOR Inhibitor-12 has been shown to possess reduced liver toxicity, enhancing its potential for therapeutic applications in oncology.
  41. PI3K/mTOR Ligand

    PI3K/mTOR ligand-1 is a ligand targeting the PI3K/mTOR pathway, crucial for cell growth and metabolism regulation. It functions as a building block for the synthesis of PROTACs aimed at modulating PI3K/mTOR signaling. This compound is valuable in cancer research and drug discovery efforts focusing on targeted protein degradation and pathway inhibition.
  42. mTOR Inhibitor

    PT-88 is a highly selective inhibitor of the mTOR (Mammalian Target of Rapamycin) pathway, demonstrating an IC50 of 1.2 nM. This compound effectively inhibits both mTORC1 and mTORC2 complexes, which play critical roles in regulating cell growth, proliferation, and survival. PT-88 is suitable for investigating the involvement of mTOR in tumorigenesis and development, particularly in breast cancer research.
  43. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-8 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. This compound promotes apoptosis in HCT-116 cells and effectively induces cell cycle arrest at the G1/S phase. It serves as a valuable tool for researchers investigating the roles of PI3K and mTOR signaling in cancer biology and potential therapeutic interventions.
  44. mTOR Inhibitor

    YB-3-17 is a bifunctional PROTAC molecule that targets the mechanistic target of rapamycin (mTOR) with an IC50 of 0.22 nM and induces degradation of G1 to S phase transition 1 gene (GSPT1) with a DC50 of 5 nM. This compound demonstrates significant antiproliferative effects in various glioblastoma cell lines, achieving nanomolar IC50 values. Additionally, YB-3-17 exhibits notable antitumor efficacy in preclinical mouse models, making it a valuable tool for studying mTOR inhibition and its implications in cancer therapy.
  45. mTOR Inhibitor

    CC214-1 is a potent mTOR inhibitor with an IC50 of 0.002 μM that induces autophagy. This compound serves as a valuable in vitro tool for investigating mTOR kinase biology. CC214-1 is particularly relevant for research in glioblastoma, providing insights into cancer cell metabolism and potential therapeutic strategies.
  46. PI3K Inhibitor

    MCX 28 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) pathway, functioning as a triple inhibitor of PI3K, mTOR, and PIM kinases. It exhibits low nanomolar activity, making it a valuable tool for studying signaling pathways involved in cancer and other diseases. This compound is particularly useful for research applications focused on the modulation of cell proliferation, survival, and metabolic processes.
  47. mTOR-C1 Inhibitor

    LGB321 is a selective mTOR-C1 inhibitor that effectively disrupts PIM2-dependent signaling pathways in multiple myeloma cell lines. This compound inhibits cell proliferation and modulates key cellular processes, including the phosphorylation of BAD. LGB321 is valuable for research focused on understanding the mechanisms of multiple myeloma and the mTOR signaling pathway.
  48. PI3K/mTOR Inhibitor

    PI3K/mTOR-IN-18 is a highly selective dual inhibitor targeting PI3Kα and mTOR, with binding affinities of Ki=0.130 nM and Ki=0.111 nM, respectively. This compound effectively blocks the PI3K/AKT/mTOR signaling pathway, resulting in significant inhibition of tumor cell proliferation (IC50=144 nM). PI3K/mTOR-IN-18 is suitable for research involving various solid tumors, including breast cancer and non-small cell lung cancer (NSCLC).
  49. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-14 is a dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), exhibiting IC50 values of 171.4 nM and 10.1 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its inhibition of the PI3K/mTOR signaling pathway can be critical for studies focused on cell proliferation and survival in various cancer models.
  50. PI3K/mTOR Inhibitor

    PI3K/mTOR Inhibitor-7 (Compound 19i) is a potent dual inhibitor targeting the PI3K and mTOR pathways. It demonstrates a 4.7-fold increased potency compared to the positive control gedatolisib, with an IC50 of 0.3 μM. At a concentration of 10 μM, PI3K/mTOR Inhibitor-7 effectively suppresses the PI3K/Akt/mTOR signaling pathway. This compound is valuable for research applications focused on cancer biology and related therapeutic development.

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