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mTOR

The mammalian target of rapamycin (mTOR), sometimes also referred to as the mechanistic target of rapamycin and FK506-binding protein 12-rapamycin-associated protein 1 (FRAP1), is a kinase that in humans is encoded by the MTOR gene. mTOR is a member of the phosphatidylinositol 3-kinase-related kinase family of protein kinases.mTOR links with other proteins and serves as a core component of two distinct protein complexes, mTOR complex 1 and mTOR complex 2, which regulate different cellular processes. In particular, as a core component of both complexes, mTOR functions as a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription. As a core component of mTORC2, mTOR also functions as a tyrosine protein kinase that promotes the activation of insulin receptors and insulin-like growth factor 1 receptors. mTORC2 has also been implicated in the control and maintenance of the actin cytoskeleton.

  • Rapamycin
    T153753123-88-9
    Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
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  • NV-5138
    T122702095886-80-7In house
    NV-5138 is a selective and orally active activator of brain mTORC1, with antidepressant effects.
    • $91
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  • Capivasertib
    T19201143532-39-1
    Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.
    • $34
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  • mTOR/HDAC-IN-1 HCl
    T63399L In house
    mTOR/HDAC-IN-1 HCl is a potent dual inhibitor of mTOR and HDAC with potential anti-inflammatory, anti-proliferative, autophagy and apoptosis-inducing effects for cancer research.
    • $195
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  • Desmethyl-VS-5584
    T41991246535-95-4
    Desmethyl-VS-5584 is a dimethyl analog of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
    • $54
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  • mTOR inhibitor 9b
    T677031144075-34-2In house
    mTOR inhibitor 9b is an enzyme inhibitor of protein kinase mTOR he phosphatidylinositol 3-kinase PIK3CA with IC50s of 0.76 nm and 1.262 µM, respectively.mTOR inhibitor 9b possesses anticancer activity and can be used to study leukemia, skin, breast, lung and colon cancers.
    • $350
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  • mTOR inhibitor 9f
    T677011144075-42-2In house
    mTOR inhibitor 9f is a selective mTOR inhibitor with IC50 of 1.25nM and 82nM for mTOR and PI3Kα, respectively.
    • $197
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  • CC214-1
    T93141021920-32-0In house
    CC214-1 is an mTOR inhibitor with potential anticancer activity, inhibits protein translation, and induces autophagy. CC214-1 is an in vitro tool compound for exploring the biology of mTOR kinases and can be used to study myeloma.
    • $195 TargetMol
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  • P-2281
    T282851112994-35-0
    P-2281 is an mTOR inhibitor with anticancer and anti-inflammatory properties.P-2281 inhibits dextran sulfate sodium (DSS)-induced colitis by suppressing T-cell function and is effective in a mouse model of human colitis.
    • $195
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  • mTOR inhibitor 9d
    T677021144075-38-6In house
    mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.
    • $350
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  • mTOR inhibitor 13
    T93101144075-44-4In house
    mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.
    • $329
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  • Insecticidal agent 364
    T67914556055-08-4
    Insecticidal agent 364 is a selective small molecule inhibitor of rapamycin kinase target protein. Insecticidal agent 364 has antitumor activity, and by inhibiting mTOR, Insecticidal agent 364 aims to disrupt signaling pathways involved in cancer cell growth and survival, thereby potentially inhibiting tumor growth.
    • $195
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  • mTOR inhibitor 9e
    T677041144075-40-0In house
    mTOR inhibitor 9e is a selective mTOR inhibitor with IC50 of 0.68nM and 1359nM for mTOR and PI3Kα, respectively.
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  • α-Hydroxyglutaric Acid Lithium
    T36624L In house
    α-Hydroxyglutaric Acid Lithium, converted from glutamate in microorganisms and animals, is an inhibitor of α-ketoglutarate-dependent dioxygenase and 5-methylcytosine hydroxylase, and has an inhibitory effect on ATP synthase and mTOR signaling.
    • $34
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  • PI3Kα/mTOR-IN-1
    T125891013098-90-2In house
    PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα in a cell free assay , respectively.
    • $656
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  • DMH-25
    T85691685280-21-0
    DMH25 is a novel covalent and potent inhibitor of mTOR and shows in vivo antitumor activity against triple-negative breast cancer cells.
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  • ElteN378
    T99501421366-99-5
    ElteN378 is a highly potent synthetic inhibitor of FKBP12 with Ki of 0.5 nM, a low atomic weight ligand with affinity comparable to that of the macrolide Rapamycin.
    • $195
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  • mTOR inhibitor 9c
    T677061144075-36-4In house
    mTOR inhibitor 9c is a selective mTOR inhibitor with IC50 of 0.7nM and 825nM for mTOR and PI3Kα, respectively.
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  • MKC-1
    T9831125313-92-0In house
    MKC-1 (Ro-31-7453) is an orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in
    • $52
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  • WYE-132
    T63461144068-46-1In house
    WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
    • $39
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  • Autogramin-1
    T104132375541-73-2In house
    Autogramin-1 potently inhibits autophagy induced by either mTORC1 inhibition (Rapamycin; IC50: 0.44 μM) or starvation (IC50: 0.17 μM).
    • $139
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  • PI3K/Akt/mTOR-IN-2
    T605642757804-89-8In house
    PI3K/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor.PI3K/Akt/mTOR-IN-2 has anticancer effects and is selective for MDA-MB-231 cells with an IC50 of 2.29 μM.PI3K/Akt/mTOR-IN-2 exhibits anticancer activity and induces cycle arrest and apoptosis in cancer cells. PI3K/Akt/mTOR-IN-2 has anticancer activity and can induce cycle arrest and apoptosis in cancer cells.
    • $33
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  • PKI-402
    T36561173204-81-3In house
    PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.
    • $30
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  • GDC-0349
    T65101207360-89-1In house
    GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
    • $33
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  • WAY-600
    T67301062159-35-6In house
    WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
    • $32
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  • Cbz-B3A
    T148861884710-81-9In house
    Cbz-B3A is a potent inhibitor of mTORC1 signalling, inhibits phosphorylation of eIF4E-binding protein 1 (4EBP1) and blocks translation by 68%.
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  • mTOR inhibitor-3
    T121231207358-59-5In house
    mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.
    • $67
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  • BGT226
    T6072L915020-55-2In house
    BGT226 (NVP-BGT226) is a novel dual PI3K / mTOR inhibitor, it acts on PI3K α/β/γ with IC50 of 4 nM / 63 nM / 38 nM, respectively.
    • $48
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  • PF-04979064
    T73431220699-06-8In house
    PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor(Ki of 0.13 nM and 1.42 nM,respectively).
    • $31
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  • hSMG-1 inhibitor 11j
    T88841402452-15-6
    hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
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  • 3BDO
    T14033890405-51-3
    3BDO is an activator of mTOR. It can also inhibit autophagy..
    • $39
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  • GSK-25
    T4488874119-56-9
    GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
    • $39
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  • AZD-8055
    T18591009298-09-2
    AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
    • $36
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  • Dactolisib Tosylate
    T145521028385-32-1
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor that targets PI3K and mTOR. dactolisib Tosylate exhibits IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. dactolisib Tosylate inhibits mTORC1 and mTORC2.
    • $42
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  • PP121
    T24151092788-83-4
    PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
    • $51
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  • PF-04691502
    T62511013101-36-4
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.
    • $30
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  • Copanlisib dihydrochloride
    T149981402152-13-9
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ). Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
    • $47
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  • Everolimus
    T1784159351-69-6
    Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
    • $37
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  • Palomid 529
    T2706914913-88-5
    Palomid 529 (SG 00529) has been used in trials studying the treatment of Age-Related Macular Degeneration.
    • $47
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  • Dactolisib
    T2235915019-65-7
    Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
    • $39
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  • OSI-027
    T6319936890-98-1
    OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
    • $35
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  • XL388
    T60301251156-08-7
    XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
    • $38
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  • Tacrolimus
    T2144104987-11-3
    Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
    • $38
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  • Torin 2
    T61001223001-51-1
    Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM/ATR/DNA-PK inhibition is 28 nM/35 nM/118 nM, respectively.
    • $35
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  • Dihydromyricetin
    T299827200-12-0
    Dihydromyricetin (Ampelopsin) is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyricetin can activate autophagy by inhibiting mTOR signaling.
    • $39
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  • KU-0063794
    T2475938440-64-3
    KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
    • $52
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  • Rotundic acid
    T5S050620137-37-5
    Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.
    • $30
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  • Polyphyllin I
    T389550773-41-6
    Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.
    • $52
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  • Torin 1
    T60451222998-36-8
    Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
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  • Ridaforolimus
    T6334572924-54-0
    Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
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