PI3K/Akt/mTOR

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  1. AKT1 Inhibitor

    Akt1-IN-8 is a selective inhibitor of AKT1 kinase, demonstrating high potency with an IC50 of 8.8 nM. This compound exhibits significant antiproliferative activity against PC-3 prostate cancer cells, with an IC50 of 3.0 μM. Akt1-IN-8 effectively reduces levels of phosphorylated GSK3β, making it a valuable tool for studying AKT signaling pathways in cancer research and therapeutic development.
  2. Akt Inhibitor

    WF-10129 is a cytotoxic steroidal compound isolated from the plant Physalis. WF-10129 inhibits liver cancer cell proliferation, induces apoptosis, interferes with metabolism, and significantly reduces lactate production in vitro and in vivo. WF-10129 can also exert anti-tumor activity by regulating the expression of related genes and proteins through the AKT-p53 pathway.
  3. PI3K/AKT Inhibitor

    PI3K/AKT-IN-3 is a selective inhibitor of the PI3K/AKT signaling pathway, known to induce both autophagy and apoptosis in various cell types. This compound is primarily utilized in cancer research to study the effects of PI3K/AKT inhibition on tumor growth and cell survival mechanisms. Its application extends to exploring therapeutic strategies targeting this critical signaling pathway in cancer treatment.
  4. Akt1 Inhibitor

    Akt1-IN-6 is a potent Akt1 inhibitor with an IC50 of less than 15 nM. This compound selectively targets the Akt1 kinase, disrupting downstream signaling pathways involved in cell survival and metabolism. It is primarily used in research applications focused on cancer biology, metabolism, and other Akt-related pathways. Its high specificity for Akt1 makes it a valuable tool for studying the roles of this kinase in various disease processes.
  5. Akt Inhibitor

    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone is a potent Akt inhibitor derived from Indigofera ovata. This compound effectively disrupts the PI3K/AKT and NF-κB signaling pathways, leading to the inhibition of cancer cell invasion and migration. Its biological activity supports research applications in cancer therapeutics and molecular signaling studies.
  6. Akt3 Inhibitor

    Akt3 ligand-1 is a potent inhibitor of Akt3, exhibiting an IC50 of 0.1 nM. This compound serves as a ligand for the development of PROTAC strategies targeting Akt3, facilitating targeted protein degradation. Akt3 ligand-1 is invaluable for research into cancer biology and cellular signaling pathways where Akt3 plays a pivotal role. Additionally, it can be utilized to synthesize PROTAC Akt3 Degrader-1, enabling further exploration of therapeutic potentials in oncological studies.
  7. Akt1 Inhibitor

    Akt1-IN-7 is a potent Akt1 inhibitor with an IC50 value of less than 15 nM. It effectively hinders the activity of Akt1, a key player in cell survival and growth signaling pathways. This compound is utilized in research focused on cancer biology, metabolic disorders, and other conditions where Akt1 signaling is implicated. Its selective inhibition of Akt1 makes it a valuable tool for elucidating the role of this kinase in various biological processes.
  8. Akt Inhibitor

    Monosialoganglioside GM3 (bovine) is a ganglioside that functions as an Akt inhibitor, impacting both VEGFR2 and Akt signaling pathways. At a concentration of 20 μM, it effectively inhibits angiogenesis and decreases the proliferation and migration of human umbilical vein endothelial cells (HUVECs). Additionally, it protects against ferroptosis, which is relevant in the context of abdominal aortic aneurysm formation, and impairs insulin signaling by disrupting the insulin receptor-Caveolin-1 complex, contributing to insulin resistance in adipocytes. This reagent is applicable in cancer and metabolic disease research.
  9. AKT1-E17K Inhibitor

    Akt1-IN-4 is a selective inhibitor of the AKT1-E17K mutant with an IC50 value of less than 15 nM. This compound effectively disrupts the activity of the AKT signaling pathway, which is implicated in various cancers. Akt1-IN-4 is suitable for research applications focused on studying the role of AKT1 mutations in tumorigenesis and therapeutic resistance.
  10. Akt Inhibitor

    Puquitinib is a selective Akt inhibitor that effectively disrupts the PI3K/AKT/mTOR signaling pathway, promoting autophagy in nasopharyngeal carcinoma cells. This compound demonstrates a dose-dependent antiproliferative effect on CNE-2 cells, which is accompanied by increased autophagosome and autolysosome formation as confirmed by fluorescence and electron microscopy. Puquitinib enhances the conversion of LC3-I to LC3-II and elevates beclin 1 levels while decreasing p62 expression. Additionally, it induces apoptosis in CNE-2 cells, highlighting the interplay between autophagy and apoptosis in mediating cell death processes relevant to cancer research.
  11. PI3Kδ Inhibitor

    PI3Kδ-IN-24 is a highly selective inhibitor of the phosphoinositide 3-kinase delta (PI3Kδ) with an IC50 of 0.1 nM. This compound demonstrates notable antiproliferative effects in cancer cell lines with elevated PI3Kδ expression. By inhibiting PI3Kδ, PI3Kδ-IN-24 effectively lowers phosphorylated AKT levels and promotes cell cycle arrest and apoptosis in tumor cells. Its applications are particularly relevant in cancer research, including studies involving diffuse large B-cell lymphoma (DLBCL).
  12. Akt Inhibitor

    TAT-TCL1-Akt-in is an Akt inhibitor that selectively modulates the Akt signaling pathway, which is crucial for cell proliferation and survival. By inhibiting Akt activity, this compound can effectively impact various cellular processes linked to tumorigenesis and cancer progression. TAT-TCL1-Akt-in is useful for research applications focused on cancer biology, signaling pathways, and therapeutic interventions targeting the Akt pathway.
  13. AKT Inhibitor

    BI-69A11 is a selective AKT inhibitor that effectively suppresses the phosphorylation of AKT, disrupting the signaling pathways associated with cell survival and proliferation. This compound demonstrates significant anticancer activity, promoting apoptosis in melanoma and prostate tumor cells. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the AKT pathway.
  14. mTOR/PI3/AKT Inhibitor

    Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells.
  15. AKT Inhibitor

    AKT-IN-7 (compound 1-P1) is a potent AKT inhibitor. AKT-IN-7 has the potential for cancer research.
  16. PI3Kδ Inhibitor

    X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
  17. PI3K/Akt/FoxO3a Inhibitor

    RLX hydrochloride is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, which plays a critical role in cellular growth and survival. This compound demonstrates significant therapeutic potential in experimental colon cancer by modulating the tumor microenvironment and enhancing the efficacy of cancer immunotherapy. Additionally, RLX hydrochloride can improve the retention of therapeutic agents within tumors when utilized with advanced nanoparticle delivery systems. It may also be effectively combined with other treatment modalities, such as chemotherapy and radiotherapy, to optimize overall cancer therapy outcomes.
  18. AKT Inhibitor

    AKT-IN-9 is a potent inhibitor of AKT (Protein Kinase B), a key regulator of the PI3K/AKT/mTOR signaling pathway. This compound plays a critical role in processes such as cell growth, survival, differentiation, and metabolism. AKT-IN-9 is valuable for research applications focusing on breast and prostate cancer, contributing to a better understanding of tumor biology and potential therapeutic strategies.
  19. Tubulin/AKT1 Inhibitor

    Tubulin/AKT1-IN-1 is an inhibitor of tubulin polymerization and AKT pathway activation. This compound demonstrates significant inhibition of proliferation and metastasis in H1975 cells, along with a modest induction of apoptosis. Tubulin/AKT1-IN-1 is particularly relevant for research in non-small cell lung cancer (NSCLC), providing a valuable tool for studying therapeutic strategies against this malignancy.
  20. PI3K Inhibitor

    PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research.
  21. Akt Inhibitor

    AKT-IN-12 is a selective Akt kinase inhibitor, exhibiting an IC50 value of 0.55 μM. It effectively induces G0/G1 cell cycle arrest and promotes apoptosis in target cells. Additionally, AKT-IN-12 inhibits phosphorylated AKT and ERK while activating JNK and phosphorylated JNK, making it a valuable reagent for research applications in leukemia studies.
  22. AKT Inhibitor

    AKT-IN-20 is a selective inhibitor of the AKT kinase, a key regulator in numerous signaling pathways involved in cell growth, survival, and metabolism. This compound effectively impedes AKT activity, making it valuable for the study of cancer mechanisms and the exploration of potential therapeutic strategies. Its application is essential for researchers investigating the role of AKT in tumorigenesis and treatment resistance.
  23. PKM2/PDK1 Inhibitor

    PKM2/PDK1-IN-1 is a dual inhibitor targeting pyruvate kinase M2 (PKM2) and pyruvate dehydrogenase kinase 1 (PDK1). It demonstrates significant biological activity by inhibiting the proliferation of non-small cell lung cancer (NSCLC) cells and inducing apoptosis. This compound promotes intercellular reactive oxygen species (ROS) production and modulates apoptotic proteins, engaging both mitochondrial and death receptor pathways in cancer cell death. Its unique mechanism makes it a valuable tool for research in cancer biology and therapeutic development.
  24. PI3K Inhibitor

    PI3K-IN-29 is a potent inhibitor of Phosphoinositide 3-kinase (PI3K), effectively disrupting the PI3K/Akt signaling pathway. It demonstrates significant cytotoxic activity against various cancer cell lines, including U87MG, HeLa, and HL60, with IC50 values of 0.264 µM, 2.04 µM, and 1.14 µM, respectively. This compound is valuable for research applications involving cancer biology and therapeutic interventions targeting the PI3K pathway.
  25. Akt Inhibitor

    Ipatasertib tosylate is a potent and selective ATP-competitive inhibitor of pan-Akt, exhibiting IC50 values of 5, 18, and 8 nM for Akt1, Akt2, and Akt3, respectively. By inhibiting Akt, Ipatasertib tosylate activates FoxO3a and NF-κB, resulting in p53-independent activation of PUMA and subsequent apoptosis in cancer cells. This compound demonstrates significant anti-tumor activity in xenograft mouse models, making it a valuable tool for cancer research and therapeutic development.
  26. AKT Inhibitor

    AKT-IN-22 is a potent allosteric inhibitor of AKT, a key kinase involved in various cellular processes such as proliferation, survival, and glucose metabolism. Its inhibition of AKT has demonstrated significant anticancer effects, making it a valuable tool for cancer research. This compound is particularly useful for studying the mechanisms of AKT signaling pathways and exploring therapeutic strategies in oncology.
  27. Akt Inhibitor

    Doxazosin hydrochloride is an Akt inhibitor that primarily targets postsynaptic α1-adrenoceptors in vascular smooth muscle. This compound exhibits vasodilatory effects, resulting in decreased peripheral vascular resistance, and is utilized in studies of hypertension and prostate hyperplasia. Additionally, Doxazosin hydrochloride has demonstrated the ability to inhibit the proliferation and migration of hepatic stellate cells in mouse liver fibrosis models, influencing fibrosis, autophagy, and apoptosis mechanisms through the activation of the PI3K/Akt/mTOR signaling pathway. It also disrupts autophagic flux, leading to enhanced apoptosis in hepatic stellate cells.
  28. Akt Inhibitor

    AKT-IN-25 is a selective inhibitor of Akt that targets its phosphorylation, thereby disrupting the PI3K/Akt/mTOR signaling pathway. This compound effectively arrests the cell cycle at the G1 phase and inhibits the migration and proliferation of pancreatic cancer cells, including PANC-1, PATU-T, and SUIT-2, with IC50 values of 3.05 μM, 1.32 μM, and 3.85 μM, respectively. AKT-IN-25 is a valuable tool for studying Akt-mediated cellular processes and therapeutic strategies in cancer research.
  29. PI3K/Akt Inhibitor

    Acetyl-Exenatide is an acetylated derivative of Exenatide, targeting the PI3K/Akt signaling pathway. This compound exhibits insulin-mimetic properties and is instrumental in type 2 diabetes research. Acetyl-Exenatide promotes Th17 differentiation while inhibiting Treg differentiation, and downregulates the phosphorylation of PI3K/Akt/FoxO1, making it a valuable tool for elucidating mechanisms underlying metabolic disorders.
  30. AKT Inhibitor

    SH-5 is a potent inhibitor of the AKT signaling pathway. It enhances apoptosis triggered by tumor necrosis factor (TNF) and effectively blocks NF-kB activation induced by TNF-α, lipopolysaccharide, phorbol ester, and cigarette smoke. This compound is valuable for research applications involving cell survival, inflammation, and cancer biology.
  31. PI3K p110α Inhibitor

    VVD-484 is a selective inhibitor targeting PI3K p110α, exhibiting an IC50 of 0.59 μM against human targets. Classified as a "silent ligand," it forms a covalent bond with Cys242 of PI3K p110α, maintaining the p110α-KRASG12C interaction. VVD-484 effectively inhibits AKT phosphorylation at S473 via a RAS-independent pathway, making it a valuable tool in the research of HER2-overexpressing cancers.
  32. PI3K Inhibitor

    PI3K-IN-56 is a potent and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K), exhibiting oral bioavailability. This compound effectively blocks the production of phosphatidylinositol-3,4,5-triphosphate (PIP3) and disrupts downstream AKT signaling pathways. Its potential applications in cancer research make PI3K-IN-56 particularly valuable for studies focusing on PI3Kα-driven malignancies, including breast and ovarian cancers.
  33. Topo-IIα/Akt Inhibitor

    NISC-6 is a dual inhibitor of Topoisomerase IIα and Akt, demonstrating significant inhibitory activity in various cancer cell lines, including UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM). This compound effectively induces both early and late apoptosis in a dose-dependent manner. NISC-6 is suitable for research focusing on melanoma and related therapeutic mechanisms.
  34. PI3K/Akt/mTOR Inhibitor、MAPK Inhibitor、NF-κB Inhibitor

    Calebin A is a potent inhibitor of the PI3K/Akt/mTOR pathway, as well as MAPK and NF-κB signaling pathways. It exhibits significant anti-tumor activity through epigenetic regulation and can suppress apoptosis while inhibiting autophagy. Additionally, Calebin A modulates adipogenesis, enhances thermogenic processes, and supports gut microbiota. This compound is suitable for research in various domains, including osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.
  35. AKT1 Inhibitor

    AKT1-IN-11 is a dual inhibitor targeting both AKT1 and tubulin, derived from Podophyllotoxin. This compound effectively down-regulates the phosphorylation of AKT kinase in tumor cells, leading to inhibited cell proliferation, a G2/M phase arrest, and the induction of apoptosis. Additionally, AKT1-IN-11 promotes tubulin depolymerization, making it a valuable tool for research into colorectal cancer and potential therapeutic strategies.
  36. Akt1 Inhibitor

    Akt1-IN-5 is a potent Akt1 inhibitor with an IC50 of less than 15 nM. This compound selectively targets the Akt1 signaling pathway, which is crucial in regulating cell survival, metabolism, and proliferation. It is primarily used in cancer research to explore the therapeutic potential of modulating Akt1 activity in various tumor types.
  37. AKT1/PKA Inhibitor

    Akt1&PKA-IN-2 (Compound R-29) is a AKT1 and PKA inhibitor with selectivity for CDK2, with IC50 values of 0.007 and 0.01 μM, respectively. Akt1&PKA-IN-2 is applicable for cancer research.
  38. Akt/p70S6K Inhibitor

    XL-418 is a potent dual inhibitor of Akt and p70S6K, demonstrating IC50 values of 1 nM for Akt1 and 2 nM for p70S6K. This compound effectively inhibits the phosphorylation of ribosomal protein S6 and GSK3β, making it a valuable tool in cancer research. XL-418 is particularly relevant for studies involving prostate carcinoma and breast cancer, contributing to the understanding of signaling pathways in tumorigenesis.
  39. AKT Inhibitor

    AKT-IN-23 is a selective inhibitor of the AKT kinase, a crucial component in the PI3K/AKT signaling pathway. This compound effectively inhibits AKT activity, leading to decreased cell proliferation and survival in various cancer cell models. AKT-IN-23 is useful in cancer research, particularly in studies focused on the modulation of signaling pathways associated with tumor progression and therapeutic resistance.
  40. Akt Inhibitor

    Hu7691 free base is a selective inhibitor of AKT, demonstrating IC50 values of 4.0 nM, 97.5 nM, and 28 nM for AKT1, AKT2, and AKT3, respectively. This compound exhibits significant antitumor activity and has been shown to reduce cutaneous toxicity in murine models. Hu7691 free base is valuable in research focused on cancer therapeutics and the modulation of the AKT signaling pathway.
  41. AKT Inhibitor

    AT7867 hydrochloride is a potent inhibitor of AKT and p70 S6 kinase, exhibiting strong oral activity. This compound demonstrates significant anticancer properties, making it a valuable tool in cancer research. Its efficacy in targeting critical signaling pathways involved in cellular growth and survival supports its use in exploring therapeutic strategies for various malignancies.
  42. Allosteric Akt Inhibitor

    MK-2206 free base is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8 nM, 12 nM, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer properties, particularly against breast cancer cell lines, as well as those harboring PIK3CA mutations and PTEN loss. MK-2206 free base is valuable for research applications focused on cancer biology and therapeutic development targeting the Akt pathway.
  43. Akt1/Akt2 Inhibitor

    AKT-IN-5 is a selective inhibitor of Akt1 and Akt2, exhibiting IC50 values of 450 nM and 400 nM, respectively. This compound has been shown to effectively modulate the Akt signaling pathway, which plays a critical role in cell survival, proliferation, and metabolism. AKT-IN-5 is valuable for research applications focused on cancer biology, metabolic disorders, and other conditions driven by aberrant Akt activity.
  44. PI3Kδ Inhibitor

    PI3Kδ-IN-10 is a potent and orally bioavailable inhibitor of the PI3Kδ enzyme, exhibiting an IC50 value of 2 nM. This compound effectively inhibits the downstream AKT signaling pathway, leading to the induction of apoptosis in hepatocellular carcinoma models. Due to its mechanism of action, PI3Kδ-IN-10 is valuable for investigating the role of PI3Kδ in cancer biology and therapeutic development.
  45. AKT/mTOR/p70S6K Inhibitor

    22-(4′-py)-JA is a semisynthetic derivative of junamycin A, primarily targeting the AKT/mTOR/p70S6K signaling pathway. This compound exhibits significant antimetastatic activity by inhibiting tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC). Furthermore, 22-(4′-py)-JA downregulates key factors including metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer properties make it a valuable tool for research, particularly in non-small cell lung cancer (NSCLC) studies.
  46. RLX

    PI3K/Akt/FoxO3a Inhibitor

    RLX (PD 139530) is a potent inhibitor of the PI3K/Akt/FoxO3a signaling pathway, exhibiting significant therapeutic potential in colon cancer models. This compound can effectively modulate the tumor microenvironment, thereby enhancing the efficacy of cancer immunotherapy. Additionally, RLX improves the retention time of therapeutic agents in tumors through advanced nanoparticle delivery systems and can be combined with various treatment modalities, such as chemotherapy and radiotherapy, to synergistically enhance cancer treatment outcomes.
  47. Dual PI3K/mTOR Inhibitor

    DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer.
  48. PI3K Inhibitor

    Zandelisib hydrochloride is a selective, non-covalent inhibitor of PI3Kδ, known for its oral bioavailability. By effectively inhibiting AKT phosphorylation, Zandelisib hydrochloride disrupts downstream signaling pathways, making it a valuable tool for investigating the role of the PI3K pathway in various malignancies. This compound is particularly relevant in research focused on relapsed and refractory B-cell lymphoma, enabling studies on tumor behavior and therapeutic responses.
  49. AKT Inhibitor

    AKT-IN-14 is a highly potent inhibitor of AKT, demonstrating IC50 values of less than 0.01 nM for AKT1, 1.06 nM for AKT2, and 0.66 nM for AKT3. This compound is primarily utilized in cancer research, providing valuable insights into AKT signaling pathways and therapeutic interventions. Its exceptional specificity and efficacy make it a crucial tool for investigating the role of AKT in tumorigenesis and cancer progression.
  50. PI3K/AKT Inhibitor

    PI3K/AKT-IN-5 is a selective inhibitor of the PI3K/AKT signaling pathway. It demonstrates potent anti-cancer activity, particularly in colorectal cancer models, by significantly inhibiting cell colony formation, inducing G2/M phase cell cycle arrest, and promoting apoptosis. This compound serves as a valuable tool for research into the mechanisms of colorectal cancer progression and treatment.

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