PI3K/Akt/mTOR

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  1. mTOR Inhibitors

    Rapamycin (Sirolimus) prevents activation of T cells and B-cells by inhibiting their response to interleukin-2 (IL-2).
  2. ATM inhibitor

    AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.
  3. GSK3 inhibitor

    AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.
  4. mTORC1/2 inhibitor

    AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor.
  5. MAO-B inhibitor

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

    FK-506 is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It reduces interleukin-2 (IL-2) production by T-cells.
  7. PI3K inhibitor

    BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
  8. PDK-1 inhibitor

    OSU-03012 is a novel celecoxib derivative, without cyclooxygenase-2 inhibitory activity, capable of inducing apoptosis in various cancer cells types.
  9. GSK-3 Inhibitor

    Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy
  10. PI3K inhibitor

    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
  11. PI3K inhibitor

    Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).

  12. AKT Inhibitor

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively.
  13. AMPK inhibitor

    BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.
  14. ATM/ATR inhibitor

    VE-821 is a potent and selective inhibitor of protein kinase ATR.
  15. S6 Kinase inhibitor

    BI-D1870 is a potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10?€?30 nM.
  16. MELK inhibitor

    OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
  17. GSK-3 inhibitor

    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.
  18. PI3K Inhibitor

    XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.
  19. PI3K/mTOR Inhibitor

    PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.
  20. PI3K/mTOR inhibitor

    Gedatolisib (PKI-587) is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.

     
  21. PTEN Inhibitor

    Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.
  22. PI3K/mTOR Dual Inhibitor

    Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).

  23. mTOR Inhibitor

    RapaLink-1 is a third-generation bivalent inhibitor targeting the mechanistic target of rapamycin (mTOR). By combining Rapamycin with MLN0128 through an inert linker, RapaLink-1 demonstrates superior efficacy in inhibiting both wild-type and mutant forms of mTOR compared to other inhibitors. This compound effectively crosses the blood-brain barrier, promoting durable mTORC1 inhibition via FKBP12 binding. Additionally, RapaLink-1 exhibits anticancer properties and may play an antithrombotic role in antiphospholipid syndrome by enhancing autophagy.
  24. mTOR Inhibitor/Autophagy Inducer

    mTOR inhibitor-8 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), functioning through the interaction with FKBP12. This compound effectively suppresses mTOR activity and induces autophagy in A549 human lung cancer cells. It is a valuable tool for studying mTOR signaling pathways and the role of autophagy in cancer research.
  25. GSK-3β Inhibitor

    Manzamine A hydrochloride is an orally active beta-carboline alkaloid that specifically inhibits GSK-3β and CDK-5, with IC50 values of 10.2 μM and 1.5 μM, respectively. This compound demonstrates significant antimalarial and anticancer properties, with additional effects such as inhibiting vacuolar ATPases and autophagy processes in pancreatic cancer cells. Furthermore, Manzamine A hydrochloride exhibits potent activity against HSV-1, making it valuable for various research applications in cancer biology and virology.
  26. mTOR/p70s6K Inhibitor

    Zederone is a sesquiterpene that acts as an inhibitor of the mTOR/p70S6K signaling pathway. It effectively reduces ovarian cancer cell proliferation and exhibits selective inhibition of various CYP450 enzymes, notably with IC50 values of 2.9 μM for CYP2B6 and 9.2 μM for CYP2C9. Additionally, Zederone demonstrates antibacterial properties against multi-drug resistant strains of Staphylococcus aureus and has been shown to improve cognitive function while modulating gut bacterial dysbiosis. However, caution is warranted due to its hepatotoxicity, evidenced by an LD50 of approximately 223 mg/kg in mice.
  27. PI3Kδ/BET Inhibitor

    PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development.
  28. CDK/GSK3β/JNK Inhibitor

    Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation.
  29. PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator

    JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms.
  30. GSK-3β Inhibitor

    GSK-3β inhibitor 13 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) and GSK-3α, demonstrating IC50 values of 0.73 nM and 0.35 nM respectively. This orally active compound exhibits blood-brain barrier permeability and effectively reduces tau phosphorylation, with an IC50 of 58 nM. Its ability to modulate tau phosphorylation makes it valuable for research focused on neurodegenerative disorders, particularly Alzheimer's disease, by potentially mitigating the formation of neurofibrillary tangles.
  31. PI3K/PIKK Inhibitor

    PI3K/PIKK-IN-1 is a potent inhibitor of phosphoinositide 3-kinases (PI3K) and PI3-kinase-related kinases (PIKK). This compound is utilized in the development of antibody-drug conjugates (ADCs), making it valuable for therapeutic applications. It is particularly relevant in the research of various cancers, including breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer, aiding in the exploration of targeted cancer therapies.
  32. Akt/ROCK Inhibitor

    Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development.
  33. PI3Kα Inhibitor

    PI3Kα-IN-16 is a selective PI3Kα inhibitor with an IC50 value of 4.28 μM. It effectively suppresses PI3K-mediated colorectal cancer growth and migration, demonstrating its potential as a therapeutic agent. Additionally, PI3Kα-IN-16 inhibits the Wnt signaling pathway, making it a valuable tool for research in cancer biology and signaling pathways.
  34. AMPK Inhibitor

    AMPK activator 16 is a potent AMP-activated protein kinase (AMPK) activator that effectively enhances AMPK signaling. It promotes the phosphorylation of AMPK, subsequently increasing the levels of phosphorylated acetyl-CoA carboxylase (p-ACC) and phosphorylated raptor (p-raptor) in N2a cells. This compound is instrumental in studies exploring metabolic regulation and signaling pathways linked to energy homeostasis and cellular stress responses.
  35. CDK2/GSK3β Inhibitor

    Tagtociclib hydrate is a potent and selective inhibitor of cyclin-dependent kinase 2 (CDK2) and glycogen synthase kinase 3 beta (GSK3β), displaying inhibition constants of 1.16 nM and 537.81 nM, respectively. This compound demonstrates significant anti-tumor activity, particularly in cancers characterized by cyclin E1 amplification. Tagtociclib hydrate serves as a valuable research tool for studying cell cycle regulation and therapeutic strategies targeting kinase pathways in cancer biology.
  36. GSK-3β Inhibitor

    GSK-3β Inhibitor 2 is a selective and potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 1.1 nM. This compound is orally active and is capable of penetrating the blood-brain barrier, making it a valuable tool for neurological research. GSK-3β Inhibitor 2 holds potential for therapeutic applications in Alzheimer's disease and other neurodegenerative conditions by modulating signaling pathways associated with neuronal survival and function.
  37. GSK-3 Inhibitor

    PF-04802367 is a highly selective glycogen synthase kinase 3 (GSK-3) inhibitor, demonstrating an IC50 of 2.1 nM in recombinant human GSK-3β assays and 1.1 nM in ADP-Glo assays. This compound effectively inhibits both GSK-3 isoforms, GSK-3α and GSK-3β, with IC50 values of 10.0 nM and 9.0 nM, respectively, as measured by mobility shift assays. PF-04802367 is distinguished by its favorable central nervous system (CNS) properties, making it a valuable tool in neurobiological research and related therapeutic investigations.
  38. GSK3β/AβOs Inhibitor

    Cu(II)GTSM is a cell-permeable copper complex that acts as a potent inhibitor of glycogen synthase kinase 3 beta (GSK3β). This compound significantly reduces the formation of amyloid-beta oligomers (AβOs) and lowers tau phosphorylation levels, thereby influencing key pathways related to neurodegenerative diseases. Additionally, Cu(II)GTSM diminishes the abundance of amyloid-beta trimers and exhibits potential as an anticancer and antimicrobial agent, making it valuable for various research applications in disease modeling and therapeutic development.
  39. GSK3β Inhibitor

    BRD3731 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), demonstrating an IC50 of 15 nM for GSK3β and 215 nM for GSK3α. This compound exhibits significant potential in research related to post-traumatic stress disorder (PTSD), various psychiatric disorders, diabetes, and neurodegenerative diseases. Its specificity and potency make it a valuable tool for studying GSK3β-related signaling pathways and therapeutic interventions.
  40. CDKL5/GSK3 Inhibitor

    SGC-CDKL5/GSK3 is a selective inhibitor targeting CDKL5 and GSK3α/β. This compound demonstrates potent inhibition, with IC50 values of 4.6 nM for CDKL5, 24 nM for GSK3β, and 9.5 nM for GSK3α, as assessed by the NanoBRET assay. Its specificity and efficacy make it a valuable tool for investigating central nervous system diseases and related biological pathways.
  41. GSK-3β Inhibitor

    GSK-3β inhibitor 22 is a potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with an IC50 of 3.1 nM. This compound is suitable for research applications focused on neurodegenerative diseases, particularly Alzheimer's disease. It provides a valuable tool for investigating the role of GSK-3β in cellular pathways and potential therapeutic interventions in related pathologies.
  42. GSK3α/β Inhibitor

    BRD0209 is a potent and selective dual inhibitor of glycogen synthase kinase 3 alpha and beta (GSK3α/β), exhibiting IC50 values of 19 nM and 5 nM, respectively. This reversible ATP-competitive inhibitor demonstrates fast-off kinetics with a Ki of 4.2 nM. As a tricyclic pyrazolotetrahydroquinolinone compound, BRD0209 is primarily utilized in the investigation of mood disorders and related neurobiological research.
  43. GSK-3 Inhibitor

    GSK-3 Inhibitor 3 is a selective inhibitor targeting glycogen synthase kinase 3 (GSK-3) with notable brain penetration. It exhibits low nanomolar potency, with IC50 values of 0.35 nM for GSK-3α and 0.25 nM for GSK-3β. This compound effectively reduces tau protein phosphorylation at the S396 site in a triple-transgenic mouse model of Alzheimer's disease, demonstrating an IC50 of 10 nM. GSK-3 Inhibitor 3 is valuable for research into neurological diseases and related signaling pathways.
  44. GSK3 Inhibitor

    CHIR 98024 is a potent glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM. This compound modulates various signaling pathways, contributing to cellular processes such as proliferation, differentiation, and metabolism. CHIR 98024 is utilized in research exploring its therapeutic potential in neurodegenerative diseases, cancer, and other disorders associated with GSK3 dysregulation.
  45. GSK3β Inhibitor

    GSK-3β Inhibitor XI is a selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β) with a potent Ki value of 25 nM. This compound enhances glycogen synthase (GS) activity, making it valuable for investigations into metabolic disorders such as type 2 diabetes and neurodegenerative diseases, including Alzheimer’s disease. Its specificity and potency render it a useful tool for elucidating the role of GSK-3β in various biological processes and therapeutic contexts.
  46. GSK3 Inhibitor

    SAR502250 is a potent and selective ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3) with an IC50 of 12 nM for human GSK-3β. This compound is orally active and exhibits the ability to penetrate the blood-brain barrier. SAR502250 demonstrates antidepressant-like activity and is applicable for research into Alzheimer's disease and related neurological conditions.
  47. GSK3/CDK9 Inhibitor

    ABC1183 is a selective dual inhibitor targeting GSK3 and CDK9, effectively inhibiting GSK3β, GSK3α, and CDK9/cyclin T1 with IC50 values of 657 nM, 327 nM, and 321 nM, respectively. This compound exhibits notable anti-inflammatory and anti-tumor activities, making it a valuable tool for cancer research and inflammation-related studies. Its ability to modulate critical signaling pathways positions ABC1183 as a promising candidate for further investigation in therapeutic applications.
  48. GSK-3 Inhibitor

    GSK3-IN-1 is a selective inhibitor of glycogen synthase kinase 3 (GSK-3) with an IC50 value of 12 μM. This compound is involved in various signaling pathways and plays a critical role in glucose metabolism and insulin signaling. GSK3-IN-1 is particularly relevant for research applications focused on diabetes and other metabolic disorders.
  49. GSK3β Inhibitor

    GSK3β Inhibitor II is a selective inhibitor targeting glycogen synthase kinase 3 beta (GSK3β). This compound exhibits significant activity in modulating GSK3β activity, making it a valuable tool for studying signaling pathways implicated in neurodegenerative diseases such as Alzheimer’s disease. Its use facilitates research aimed at elucidating the roles of GSK3β in cellular processes and potential therapeutic strategies for AD.
  50. GSK-3/CDK5/CDK2 Inhibitor

    GSK-3/CDK5/CDK2-IN-1 is a potent inhibitor targeting GSK-3, CDK5, and CDK2. This imidazole derivative has demonstrated effectiveness in modulating pathways relevant to tumorigenesis and neurodegenerative disorders. Its ability to inhibit these kinases makes it a valuable tool for investigating mechanisms underlying cancer proliferation and neurodegeneration.

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