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Catalog No. Product Name Information Product Use Citations Product Validations
E0115 MTI-31 MTI-31 (LXI-15029) is a novel mTORC1/mTORC2 inhibitor with Kd of 0.2 nM in mTOR binding assays and displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G.
E1151New JR-AB2-011 JR-AB2-011 is a potent inhibitor of mTOR-mLST8-mSIN1-Rictor complex (mTORC2) which can block mTORC2 signaling and Rictor association with mTOR at lower effective concentrations.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
S0179 mTOR inhibitor-1 mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Theranostics, 2022, 12(9):4348-4373
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669, AP23573) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
Int J Mol Sci, 2021, 22(21)11864
bioRxiv, 2021, 2021.04.15.440067
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1039 Rapamycin (AY-22989) Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804,AY-22989) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
Nat Biotechnol, 2022, 10.1038/s41587-022-01386-z
Nat Nanotechnol, 2022, 10.1038/s41565-021-01048-2
Cancer Discov, 2022, candisc.1672.2021
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
J Immunother Cancer, 2022, 10(1)e003766
Cancer Res, 2022, canres.1397.2021
Cell Rep, 2022, 39(4):110721
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD, Afinitor) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancer Cell, 2022, S1535-6108(21)00662-0
Sci Adv, 2022, 8(29):eabm8780
S1226 KU-0063794 KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.
Cancers (Basel), 2022, 14(13)3186
PLoS Pathog, 2021, 17(1):e1009111
Sci Rep, 2021, 11(1):13302
S1266 WYE-354 WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
Cancers (Basel), 2020, 12(12)E3519
Oncol Rep, 2019, 41(6):3179-3188
Mol Ther Nucleic Acids, 2018, 11:485-493
S1360 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
Am J Cancer Res, 2022, 12(3):1102-1115
BMC Cancer, 2020, 20(1):4
Cell Rep, 2019, 27(3):820-834
S1523 Voxtalisib (XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Cell Oncol (Dordr), 2020, 8
Cell Rep, 2015, 11(3):446-59
Mol Cancer Res, 2014, 12(5):703-13
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Immunity, 2022, 55(1):159-173.e9
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Small, 2022, 18(4):e2103552
S1627 Nitazoxanide (NSC 697855) Nitazoxanide (NTZ, NSC 697855) is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Biochem Pharmacol, 2022, 197:114913
Oncol Lett, 2022, 23(4):123
Microorganisms, 2022, 10(7)1421
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Nat Commun, 2022, 13(1):1548
Cell Rep, 2022, 39(4):110721
S2238 Palomid 529 (P529) Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6. Phase 1.
J Biomed Res, 2020, 0(0):1-9
Sci Rep, 2017, 7:41718
Mol Cancer Res, 2015, 13(2):223-30
S2406 Chrysophanic Acid Chrysophanic Acid (Chrysophanol) a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
Cell Prolif, 2020, e12871
Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells. Phase 1.
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
Front Cell Dev Biol, 2021, 9:785979
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Front Oncol, 2022, 12:862806
Int J Mol Sci, 2022, 23(8)4277
Leuk Lymphoma, 2022, 63(2):404-415
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
Mol Cell, 2022, S1097-2765(22)00393-8
Nucleic Acids Res, 2022, gkac375
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Cell, 2022, S0092-8674(22)00472-X
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4077
S2661 WYE-125132 (WYE-132) WYE-125132 (WYE-132) 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.
Cancers (Basel), 2022, 14(6)1575
Br J Haematol, 2022, 10.1111/bjh.18187
Mol Cells, 2021, 44(1):50-62
S2668 WYE-687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
J Hepatol, 2015, 10.1016/j.jhep.2015.11.011
S2689 WAY-600 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).
Nat Commun, 2021, 12(1):2699
Front Cell Dev Biol, 2020, 8:383
Biochem Biophys Res Commun, 2016, 474(2):330-7
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Nat Commun, 2022, 13(1):2500
Theranostics, 2022, 12(4):1659-1682
Cancers (Basel), 2022, 14(6)1575
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Evid Based Complement Alternat Med, 2022, 2022:8110796
Cells, 2021, 10(5)1261
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
Cancer Biol Ther, 2017, 18(10):816-826
Oncotarget, 2016, 7(34):55690-55703
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Small, 2022, 18(4):e2103552
Sci Rep, 2022, 12(1):6345
Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(4):598-603
S2811 Sapanisertib (MLN0128) Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Nature, 2022, 602(7895):112-116
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Chem Biol, 2022, S2451-9456(22)00236-7
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Mol Cell, 2022, S1097-2765(22)00327-6
Autophagy, 2022, 10.1080/15548627.2022.2065617
Nat Commun, 2022, 13(1):2500
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Cycle, 2022, 1-14
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK(IC50=0.28 μM) and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells.
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
Front Pharmacol, 2021, 12:659511
S6517 GNE-493 GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
Cell Death Discov, 2022, 8(1):120
S7035 XL388 XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.
Autophagy, 2015, 11(10):1729-44
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578,A 179578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
PLoS Biol, 2019, 17(5):e3000252
PLoS Biol, 2019, 17(5):e3000252
S7369 4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.
FASEB J, 2021, 35(5):e21445
Mol Pharmacol, 2021, 99(1):1-16
J Cell Mol Med, 2021, 10.1111/jcmm.16307
S7614New MHY-1685 MHY-1685 is a novel mTOR inhibitor, which attenuates senescence by modulating autophagy through the inhibition of mTOR in human cardiac stem cells.
S7646 Voxtalisib (XL765) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Toxicol Appl Pharmacol, 2022, 437:115886
Front Immunol, 2021, 12:761326
Genome Med, 2020, 18;12(1):17
S7886 Onatasertib (CC 223) Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2.
Biochem Biophys Res Commun, 2018, 496(4):1191-1196
PLoS One, 2017, 12(3):e0173252
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.
Neoplasia, 2022, 27:100780
Cancers (Basel), 2022, 14(13)3186
Sci Rep, 2021, 11(1):20338
S8040 GDC-0349 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.
BMB Rep, 2021, 54(5):272-277
Cell Death Differ, 2020, 10.1038/s41418-020-00649-z
Biochem Biophys Res Commun, 2016, 477(2):174-80
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Nat Commun, 2019, 10(1):5718
Nat Commun, 2019, 10(1):3585
Oncogenesis, 2019, 8(7):38
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
S8298 CZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
S8738 Bimiralisib (PQR309) Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Haematologica, 2022, 10.3324/haematol.2021.279957
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cancer Cell Int, 2021, 21(1):24
S8784 PQR620 PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
E0795New COH-SR4 COH-SR4 suppresses adipogenesis in 3T3-L1 cells through indirect activation of AMPK and downstream modulation of the Mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which blocks important regulators involved in protein synthesis, cell cycle progression, and expression of key transcription factors and their target adipogenic genes involved in lipid synthesis. 
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties. Salidroside is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
FASEB J, 2021, 35(12):e22044
Curr Med Sci, 2021, 10.1007/s11596-021-2374-6
J Med Virol, 2019, 91(8):1440-1447
S3753 L-Leucine Leucine ((S)-Leucine, Leu) is one of nine essential amino acids in humans which is important for protein synthesis and many metabolic functions. It contributes to regulation of blood-sugar levels; growth and repair of muscle and bone tissue; growth hormone production; and wound healing. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Hepatology, 2022, 75(6):1386-1401
Emerg Microbes Infect, 2022, 1-85
Front Pharmacol, 2022, 13:890974
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Front Oncol, 2021, 11:665420
Exp Ther Med, 2021, 21(6):581
Mol Med Rep, 2021, 24(2)592
S1847 Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
J Clin Invest, 2022, e152187
Neuroscience, 2022, S0306-4522(22)00001-X
Neuron, 2021, S0896-6273(21)00352-4
S9514 Rotundic acid 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.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.
E2012New Ginkgolide K Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway, and possesses neuroprotective activity.
E0115 MTI-31 MTI-31 (LXI-15029) is a novel mTORC1/mTORC2 inhibitor with Kd of 0.2 nM in mTOR binding assays and displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G.
E1151New JR-AB2-011 JR-AB2-011 is a potent inhibitor of mTOR-mLST8-mSIN1-Rictor complex (mTORC2) which can block mTORC2 signaling and Rictor association with mTOR at lower effective concentrations.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
S0179 mTOR inhibitor-1 mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Theranostics, 2022, 12(9):4348-4373
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669, AP23573) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
Int J Mol Sci, 2021, 22(21)11864
bioRxiv, 2021, 2021.04.15.440067
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1039 Rapamycin (AY-22989) Rapamycin (AY-22989, Rapamune, Sirolimus, NSC-2260804,AY-22989) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
Nat Biotechnol, 2022, 10.1038/s41587-022-01386-z
Nat Nanotechnol, 2022, 10.1038/s41565-021-01048-2
Cancer Discov, 2022, candisc.1672.2021
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
J Immunother Cancer, 2022, 10(1)e003766
Cancer Res, 2022, canres.1397.2021
Cell Rep, 2022, 39(4):110721
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD, Afinitor) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancer Cell, 2022, S1535-6108(21)00662-0
Sci Adv, 2022, 8(29):eabm8780
S1226 KU-0063794 KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.
Cancers (Basel), 2022, 14(13)3186
PLoS Pathog, 2021, 17(1):e1009111
Sci Rep, 2021, 11(1):13302
S1266 WYE-354 WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
Cancers (Basel), 2020, 12(12)E3519
Oncol Rep, 2019, 41(6):3179-3188
Mol Ther Nucleic Acids, 2018, 11:485-493
S1360 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
Am J Cancer Res, 2022, 12(3):1102-1115
BMC Cancer, 2020, 20(1):4
Cell Rep, 2019, 27(3):820-834
S1523 Voxtalisib (XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Cell Oncol (Dordr), 2020, 8
Cell Rep, 2015, 11(3):446-59
Mol Cancer Res, 2014, 12(5):703-13
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Immunity, 2022, 55(1):159-173.e9
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Small, 2022, 18(4):e2103552
S1627 Nitazoxanide (NSC 697855) Nitazoxanide (NTZ, NSC 697855) is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.
Biochem Pharmacol, 2022, 197:114913
Oncol Lett, 2022, 23(4):123
Microorganisms, 2022, 10(7)1421
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Nat Commun, 2022, 13(1):1548
Cell Rep, 2022, 39(4):110721
S2238 Palomid 529 (P529) Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6. Phase 1.
J Biomed Res, 2020, 0(0):1-9
Sci Rep, 2017, 7:41718
Mol Cancer Res, 2015, 13(2):223-30
S2406 Chrysophanic Acid Chrysophanic Acid (Chrysophanol) a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
Cell Prolif, 2020, e12871
Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2624 OSI-027 OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells. Phase 1.
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
Front Cell Dev Biol, 2021, 9:785979
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Front Oncol, 2022, 12:862806
Int J Mol Sci, 2022, 23(8)4277
Leuk Lymphoma, 2022, 63(2):404-415
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
Mol Cell, 2022, S1097-2765(22)00393-8
Nucleic Acids Res, 2022, gkac375
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Cell, 2022, S0092-8674(22)00472-X
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4077
S2661 WYE-125132 (WYE-132) WYE-125132 (WYE-132) 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.
Cancers (Basel), 2022, 14(6)1575
Br J Haematol, 2022, 10.1111/bjh.18187
Mol Cells, 2021, 44(1):50-62
S2668 WYE-687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
J Hepatol, 2015, 10.1016/j.jhep.2015.11.011
S2689 WAY-600 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).
Nat Commun, 2021, 12(1):2699
Front Cell Dev Biol, 2020, 8:383
Biochem Biophys Res Commun, 2016, 474(2):330-7
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Nat Commun, 2022, 13(1):2500
Theranostics, 2022, 12(4):1659-1682
Cancers (Basel), 2022, 14(6)1575
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Evid Based Complement Alternat Med, 2022, 2022:8110796
Cells, 2021, 10(5)1261
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
Cancer Biol Ther, 2017, 18(10):816-826
Oncotarget, 2016, 7(34):55690-55703
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Small, 2022, 18(4):e2103552
Sci Rep, 2022, 12(1):6345
Nan Fang Yi Ke Da Xue Xue Bao, 2022, 42(4):598-603
S2811 Sapanisertib (MLN0128) Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Nature, 2022, 602(7895):112-116
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Chem Biol, 2022, S2451-9456(22)00236-7
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
S2827 Torin 1 Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Mol Cell, 2022, S1097-2765(22)00327-6
Autophagy, 2022, 10.1080/15548627.2022.2065617
Nat Commun, 2022, 13(1):2500
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Cell Cycle, 2022, 1-14
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK(IC50=0.28 μM) and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells.
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
Front Pharmacol, 2021, 12:659511
S6517 GNE-493 GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
Cell Death Discov, 2022, 8(1):120
S7035 XL388 XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.
Autophagy, 2015, 11(10):1729-44
S7091 Zotarolimus (ABT-578) Zotarolimus (ABT-578,A 179578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.
PLoS Biol, 2019, 17(5):e3000252
PLoS Biol, 2019, 17(5):e3000252
S7369 4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.
FASEB J, 2021, 35(5):e21445
Mol Pharmacol, 2021, 99(1):1-16
J Cell Mol Med, 2021, 10.1111/jcmm.16307
S7614New MHY-1685 MHY-1685 is a novel mTOR inhibitor, which attenuates senescence by modulating autophagy through the inhibition of mTOR in human cardiac stem cells.
S7646 Voxtalisib (XL765) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Toxicol Appl Pharmacol, 2022, 437:115886
Front Immunol, 2021, 12:761326
Genome Med, 2020, 18;12(1):17
S7886 Onatasertib (CC 223) Onatasertib (CC 223) is a potent, selective, and orally bioavailable mTOR inhibitor with IC50 of 16 nM, >200-fold selectivity over the related PI3K-α. Phase 1/2.
Biochem Biophys Res Commun, 2018, 496(4):1191-1196
PLoS One, 2017, 12(3):e0173252
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.
Neoplasia, 2022, 27:100780
Cancers (Basel), 2022, 14(13)3186
Sci Rep, 2021, 11(1):20338
S8040 GDC-0349 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.
BMB Rep, 2021, 54(5):272-277
Cell Death Differ, 2020, 10.1038/s41418-020-00649-z
Biochem Biophys Res Commun, 2016, 477(2):174-80
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Nat Commun, 2019, 10(1):5718
Nat Commun, 2019, 10(1):3585
Oncogenesis, 2019, 8(7):38
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
S8298 CZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
S8738 Bimiralisib (PQR309) Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Haematologica, 2022, 10.3324/haematol.2021.279957
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cancer Cell Int, 2021, 21(1):24
S8784 PQR620 PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.
S9611 ABTL-0812 ABTL0812 (α-Hydroxylinoleic acid, LP-10218, SCLN-0812) inhibits Akt/mTOR axis by inducing the overexpression of TRIB3 and activating autophagy in lung squamous carcinoma cell lines. ABTL0812 also induces AMPK activation and ROS accumulation.
E0795New COH-SR4 COH-SR4 suppresses adipogenesis in 3T3-L1 cells through indirect activation of AMPK and downstream modulation of the Mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which blocks important regulators involved in protein synthesis, cell cycle progression, and expression of key transcription factors and their target adipogenic genes involved in lipid synthesis. 
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties. Salidroside is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
FASEB J, 2021, 35(12):e22044
Curr Med Sci, 2021, 10.1007/s11596-021-2374-6
J Med Virol, 2019, 91(8):1440-1447
S3753 L-Leucine Leucine ((S)-Leucine, Leu) is one of nine essential amino acids in humans which is important for protein synthesis and many metabolic functions. It contributes to regulation of blood-sugar levels; growth and repair of muscle and bone tissue; growth hormone production; and wound healing. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Hepatology, 2022, 75(6):1386-1401
Emerg Microbes Infect, 2022, 1-85
Front Pharmacol, 2022, 13:890974
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Front Oncol, 2021, 11:665420
Exp Ther Med, 2021, 21(6):581
Mol Med Rep, 2021, 24(2)592
S1847 Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
J Clin Invest, 2022, e152187
Neuroscience, 2022, S0306-4522(22)00001-X
Neuron, 2021, S0896-6273(21)00352-4
S9514 Rotundic acid 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.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.
E1151New JR-AB2-011 JR-AB2-011 is a potent inhibitor of mTOR-mLST8-mSIN1-Rictor complex (mTORC2) which can block mTORC2 signaling and Rictor association with mTOR at lower effective concentrations.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
S7614New MHY-1685 MHY-1685 is a novel mTOR inhibitor, which attenuates senescence by modulating autophagy through the inhibition of mTOR in human cardiac stem cells.
E0795New COH-SR4 COH-SR4 suppresses adipogenesis in 3T3-L1 cells through indirect activation of AMPK and downstream modulation of the Mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which blocks important regulators involved in protein synthesis, cell cycle progression, and expression of key transcription factors and their target adipogenic genes involved in lipid synthesis. 
E2012New Ginkgolide K Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway, and possesses neuroprotective activity.
Tags: mTOR inhibition | mTOR cancer | mTOR activation | mTOR target | mTOR tumor | mTOR phosphorylation | mTOR activity | mTOR inhibitor drugs | mTOR kinase assay | mTOR inhibitor cancer | mTOR inhibitor therapy | mTOR signaling pathway | mTOR inhibitor review