PI3K/Akt/mTOR

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  1. 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.
  2. 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.
  3. PI3K Inhibitor

    TG100-115 inhibits PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively).
  4. 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.
  5. 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.
  6. AKT Inhibitor

    PHT-427 is a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor.
  7. 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.
  8. 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.
  9. 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).
  10. 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.
  11. 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.
  12. GSK-3 inhibitor

    CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3.
  13. 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.
  14. PI3K inhibitor

    PKI-402 is a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.
  15. 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.
  16. ATR inhibitor

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

  17. PI3K activator

    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  18. Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc.
  19. L-LEUCINE-13C6, also known as 13C6-D-Leucine or L-Leucine-1,2,3,4,5,5'-13C6, is a fully 13C labelled D-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.

  20. GSK3α inhibitor

    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor.
  21. 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).
  22. broad-spectrum seed treatment nematicide

    Tioxazafen is a disubstituted oxadiazole and a broad-spectrum seed treatment nematicide. Tioxazafen is designed to provide consistent broad-spectrum control of nematodes in corn, soy, and cotton.
  23. 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.
  24. ILK inhibitor

    ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
  25. Peptidyl-Prolyl Cis/Trans Isomerase NIMA-Interacting 1 Mouse Recombinant
  26. Peptidyl-Prolyl Cis/Trans Isomerase NIMA-Interacting 1 Human Recombinant
  27. PIN1, Mouse Anti Human
  28. PI3K Activator

    UCL-TRO-1938 is a potent allosteric activator of phosphoinositide 3-kinase alpha (PI3Kα), exhibiting an EC50 value of approximately 60 μM. This compound promotes cell proliferation and demonstrates cardioprotective effects against ischemia-reperfusion injury. Additionally, UCL-TRO-1938 enhances nerve regeneration following nerve crush, making it a valuable tool in neuroprotection and regenerative medicine research.
  29. 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.
  30. 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.
  31. 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.
  32. PI3K/Akt/CREB Activator

    PI3K/Akt/CREB activator 1 is a potent, orally active compound that stimulates the PI3K/Akt/CREB signaling pathway. This activator promotes neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like cells, and facilitates the axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. It is particularly relevant for research into vascular dementia (VaD).
  33. PI3K/AKT Inhibitor

    PI3K/AKT-IN-1 is a potent dual inhibitor of the PI3K/AKT signaling pathway, exhibiting IC50 values of 6.99 μM for PI3Kγ, 4.01 μM for PI3Kδ, and 3.36 μM for AKT. This compound demonstrates significant anticancer activity by disrupting the PI3K/AKT axis, leading to the induction of caspase-3 dependent apoptosis. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/AKT pathway.
  34. PI3K/MDK Inhibitor

    iMDK is a potent inhibitor of phosphoinositide 3-kinase (PI3K) and midkine (MDK), a growth factor associated with tumorigenesis. This compound has demonstrated the ability to effectively suppress non-small cell lung cancer (NSCLC) growth, particularly in combination with MEK inhibitors, while exhibiting minimal toxicity to normal cells and healthy mouse models. iMDK is a valuable tool for researchers studying cancer biology and potential therapeutic strategies targeting the PI3K/MDK signaling pathway.
  35. PI3Ka Inhibitor

    Zovegalisib is an orally active allosteric inhibitor that selectively targets mutant forms of PI3Kα, exhibiting significant anti-tumor activity. This compound has demonstrated efficacy in inhibiting tumor growth in PIK3CA-mutant xenograft mouse models while exhibiting minimal effects on insulin levels. It is valuable for research into targeted cancer therapies and the exploration of PI3K signaling pathways.
  36. AKT PROTAC Degrader

    MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.
  37. PROTAC AKT Degrader

    MS170 is a highly selective PROTAC degrader targeting the AKT isoforms. With a DC50 value of 32 nM, MS170 effectively depletes total AKT (T-AKT) in cellular assays. It demonstrates strong binding affinity for AKT1, AKT2, and AKT3, with dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM, respectively. This compound is suitable for research applications investigating AKT-related signaling pathways and therapeutic interventions in cancer biology.
  38. Endogenous Metabolite

    Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health.
  39. Secondary Metabolite

    Atranorin is a secondary metabolite derived from lichens that acts as an AKT inhibitor. This compound demonstrates a wide range of biological activities, including antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Notably, Atranorin has IC50 values of 117 μM for scavenging DPPH free radicals and less than 10 μM for ABTS radicals, highlighting its potent antioxidant capacity. Additionally, Atranorin promotes wound healing and can be utilized in research focused on myelodysplastic syndromes, tumors, and various inflammatory conditions.
  40. CDK Inhibitor

    Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders.
  41. CDK Inhibitor

    NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways.
  42. GSK-3α/β Inhibitor

    (E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis.
  43. Anti-Insect Agent

    Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury.
  44. Iron Chelator

    Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
  45. AMPK Agonist

    10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.
  46. PPAR Activator

    Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation.
  47. Glycosaminoglycan

    Hyaluronic acid sodium, also known as sodium hyaluronate, is a glycosaminoglycan that plays a crucial role in the extracellular matrix (ECM). This biopolymer is involved in key biological activities such as cell proliferation, tissue remodeling, and angiogenesis, particularly in the context of digestive cancers. Hyaluronic acid sodium is implicated in tumor cell growth and migration, and it activates the PI3K-Akt signaling pathway. This reagent can also be utilized in research related to joint diseases, wound healing, and as a drug delivery system to enhance the efficacy of therapeutics in cancer research.
  48. MELK Inhibitor

    HTH-01-091 is a selective inhibitor of maternal embryonic leucine zipper kinase (MELK), exhibiting an IC50 of 10.5 nM. In addition to its primary target, HTH-01-091 also demonstrates inhibitory activity against PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. This compound is valuable for research applications focused on breast cancer and elucidating the role of MELK in tumorigenesis.
  49. mTORC1 Inhibitor

    RMC-4745 is a selective dual-site inhibitor of mTORC1 with a 35-fold higher affinity for mTORC1 compared to mTORC2. It effectively inhibits the proliferation of MCF-7 breast cancer cells and induces apoptosis by upregulating Caspase-3/7 activity. Notably, RMC-4745 does not lead to the upregulation of HER3 due to its selective inhibition of mTORC2. This compound is valuable for research focused on breast cancer and the mechanisms underlying mTOR signaling.
  50. Akt Allosteric Inhibitor

    AKT-IN-28 is an allosteric inhibitor of Akt, a key protein involved in cell survival and metabolism. It exhibits a binding affinity with a Kd of 2.07 μM and demonstrates the ability to significantly inhibit Akt activity. This compound induces apoptosis, arrests the cell cycle in the G2/M phase, and suppresses proliferation, migration, and metabolic processes in KRAS mutant colorectal cancer cells, making it a valuable tool for cancer research applications focused on targeting the Akt pathway.

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