mTOR

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シグナル伝達経路

mTORシグナル伝達経路

mTOR製品

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S1039 Rapamycin (Sirolimus) ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。
Drug Resist Updat, 2024, 73:101063
Cell Rep Med, 2024, 5(2):101420
J Adv Res, 2024, S2090-1232(24)00079-1
S1120 Everolimus エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。
Cell, 2024, 187(3):712-732.e38
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
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.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
J Biol Chem, 2024, S0021-9258(24)00057-7
Nat Neurosci, 2023, none
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.
Nucleic Acids Res, 2024, gkad1224
Theranostics, 2024, 14(4):1561-1582
Genes Dev, 2024, 38(1-2):70-94
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.
Int J Chron Obstruct Pulmon Dis, 2024, 19:269-279
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
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.
Cell Metab, 2022, 34(5):667-680.e6
Cell Metab, 2022, S1550-4131(22)00191-7
Nat Struct Mol Biol, 2022, (9):863-870.
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.
Cells, 2024, 13(4)304
Transl Oncol, 2024, 43:101857
Cancer Cell, 2023, 41(1):139-163.e17
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.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Nat Commun, 2023, 14(1):390
Aging Cell, 2023, e13888.
BMC Cancer, 2023, 23(1):499
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.
Comput Struct Biotechnol J, 2023, 21:1157-1168
Mol Cell Biol, 2023, 43(1):1-21
J Cell Commun Signal, 2023, 17(3):975-989
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.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Iran J Basic Med Sci, 2024, 27(3):360-365.
J Radiat Res, 2024, rrad107
Research Square, 2024, 10.21203/rs.3.rs-3872267/v1
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.
Virulence, 2023, 14(1):2171636
Mol Biol Cell, 2023, 34(5):ar35
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
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.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
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.
J Exp Clin Cancer Res, 2023, 42(1):8
Cell Death Dis, 2023, 14(10):652
Cell Death Dis, 2023, 14(10):652
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.
Exp Gerontol, 2024, 186:112359
iScience, 2023, 26(9):107734
Exp Gerontol, 2023, 173:112091
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.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
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.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
Nat Commun, 2022, 13(1):2500
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.
Nat Commun, 2024, 15(1):686
Int J Mol Sci, 2023, 24(2)1668
Cell Rep Methods, 2023, 3(10):100599
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.
Brain Sci, 2023, 13(5)745
Brain Sci, 2023, 13(5)745
Adv Skin Wound Care, 2023, 36(5):249-258
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
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
Front Pharmacol, 2022, 13:914153
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
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
S1627 Nitazoxanide Nitazoxanide 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.
Biomed Pharmacother, 2024, 171:116195
Viruses, 2024, 16(2)282
iScience, 2022, 25(11):105342
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
Cells, 2024, 13(4)304
Mol Ther Nucleic Acids, 2023, 31:309-323
Biochim Biophys Acta Gene Regul Mech, 2023, 1866(2):194939
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.
Br J Haematol, 2022, 10.1111/bjh.18187
Cancers (Basel), 2022, 14(6)1575
Mol Cells, 2021, 44(1):50-62
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Cancers (Basel), 2024, 16(2)370
J Exp Clin Cancer Res, 2023, 42(1):99
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
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.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
S2238 Palomid 529 (P529) Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS. Phase 1.
J Biomed Res, 2020, 0(0):1-9
Sci Rep, 2017, 7:41718
Mol Cancer Res, 2015, 13(2):223-30
S8322 Samotolisib (LY3023414) LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Exp Ther Med, 2023, 25(1):19
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
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
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
mBio, 2024, e0228723.
iScience, 2023, 25(7)
Cell Rep, 2022, 41(11):111836
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
PLoS One, 2016, 11(10):e0164895
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 Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
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.
Molecules, 2023, 28(6)2820
Molecules, 2023, 28(6), 2820
PLoS Biol, 2019, 17(5):e3000252
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
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.
Mol Med Rep, 2023, 27(2)37
Research Square, 2023, 10.21203/rs.3.rs-3696850/v1
FASEB J, 2021, 35(12):e22044
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
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
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR.
Cell Death Discov, 2023, 9(1):172
Mol Cancer Res, 2022, 20(6):996-1008
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
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.
Mol Ther Nucleic Acids, 2023, 31:309-323
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
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
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
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
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
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
E1151 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.
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.
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.
E2375 PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
E2012 Ginkgolide K Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway, and possesses neuroprotective activity.
S8298 CZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
E0795 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. 
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.
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.
S0179 mTOR inhibitor-1 mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
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.
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.
S7614 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.
S1039 Rapamycin (Sirolimus) ラパマイシン (Rapamycin (Rapamune, Sirolimus, NSC-2260804,AY-22989)) は特異的 mTOR 阻害剤であり、HEK293 細胞に対する IC50 は < 0.1 nM です。
Drug Resist Updat, 2024, 73:101063
Cell Rep Med, 2024, 5(2):101420
J Adv Res, 2024, S2090-1232(24)00079-1
S1120 Everolimus エベロリムス (Everolimus (RAD001, SDZ-RAD)) は FKBP12 に結合することで形成した複合体により mTOR を阻害します。Cell-free assay における IC50 は1.6 ~ 2.4 nM です。エベロリムスは アポトーシス (apoptosis)オートファジー (autophagy) を誘発することによりがん細胞の増殖を阻害します。
Cell, 2024, 187(3):712-732.e38
Mol Metab, 2024, 80:101876
Cancer Cell, 2023, 41(1):139-163.e17
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.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
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.
Gastroenterology, 2024, S0016-5085(24)00062-3
J Biol Chem, 2024, S0021-9258(24)00057-7
Nat Neurosci, 2023, none
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.
Nucleic Acids Res, 2024, gkad1224
Theranostics, 2024, 14(4):1561-1582
Genes Dev, 2024, 38(1-2):70-94
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.
Int J Chron Obstruct Pulmon Dis, 2024, 19:269-279
Cell Discov, 2023, 9(1):92
Cell Discov, 2023, 9(1):92
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.
Cell Metab, 2022, 34(5):667-680.e6
Cell Metab, 2022, S1550-4131(22)00191-7
Nat Struct Mol Biol, 2022, (9):863-870.
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.
Cells, 2024, 13(4)304
Transl Oncol, 2024, 43:101857
Cancer Cell, 2023, 41(1):139-163.e17
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.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S1044 Temsirolimus Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Nat Commun, 2023, 14(1):390
Aging Cell, 2023, e13888.
BMC Cancer, 2023, 23(1):499
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.
Comput Struct Biotechnol J, 2023, 21:1157-1168
Mol Cell Biol, 2023, 43(1):1-21
J Cell Commun Signal, 2023, 17(3):975-989
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.
Cell Rep Med, 2023, 4(4):101007
Front Pharmacol, 2023, 14:1158775
Cancers (Basel), 2023, 15(13)3451
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.
Virulence, 2023, 14(1):2171636
Mol Biol Cell, 2023, 34(5):ar35
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
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.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
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.
J Exp Clin Cancer Res, 2023, 42(1):8
Cell Death Dis, 2023, 14(10):652
Cell Death Dis, 2023, 14(10):652
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.
Exp Gerontol, 2024, 186:112359
iScience, 2023, 26(9):107734
Exp Gerontol, 2023, 173:112091
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.
J Cell Commun Signal, 2023, 17(3):975-989
Emerg Microbes Infect, 2022, 11(1):519-531
Mol Carcinog, 2022, 10.1002/mc.23414
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.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Cell Metab, 2022, S1550-4131-2200411-9
Nat Commun, 2022, 13(1):2500
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.
Nat Commun, 2024, 15(1):686
Int J Mol Sci, 2023, 24(2)1668
Cell Rep Methods, 2023, 3(10):100599
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.
Brain Sci, 2023, 13(5)745
Brain Sci, 2023, 13(5)745
Adv Skin Wound Care, 2023, 36(5):249-258
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
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
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
S1627 Nitazoxanide Nitazoxanide 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.
Biomed Pharmacother, 2024, 171:116195
Viruses, 2024, 16(2)282
iScience, 2022, 25(11):105342
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
Cells, 2024, 13(4)304
Mol Ther Nucleic Acids, 2023, 31:309-323
Biochim Biophys Acta Gene Regul Mech, 2023, 1866(2):194939
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.
Br J Haematol, 2022, 10.1111/bjh.18187
Cancers (Basel), 2022, 14(6)1575
Mol Cells, 2021, 44(1):50-62
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Cancers (Basel), 2024, 16(2)370
J Exp Clin Cancer Res, 2023, 42(1):99
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
S2238 Palomid 529 (P529) Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS. Phase 1.
J Biomed Res, 2020, 0(0):1-9
Sci Rep, 2017, 7:41718
Mol Cancer Res, 2015, 13(2):223-30
S8322 Samotolisib (LY3023414) LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Exp Ther Med, 2023, 25(1):19
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
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
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
mBio, 2024, e0228723.
iScience, 2023, 25(7)
Cell Rep, 2022, 41(11):111836
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
PLoS One, 2016, 11(10):e0164895
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 Transplant, 2023, 32:9636897231198167
Cell Transplant, 2023, 32:9636897231198167
Cell Cycle, 2022, 1-14
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.
Molecules, 2023, 28(6)2820
Molecules, 2023, 28(6), 2820
PLoS Biol, 2019, 17(5):e3000252
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
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
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
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR.
Cell Death Discov, 2023, 9(1):172
Mol Cancer Res, 2022, 20(6):996-1008
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
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.
Mol Ther Nucleic Acids, 2023, 31:309-323
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
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
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
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
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
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
E1151 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.
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.
E2375 PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
S8298 CZ415 CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
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.
S0179 mTOR inhibitor-1 mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
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.
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.
S7614 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.
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Iran J Basic Med Sci, 2024, 27(3):360-365.
J Radiat Res, 2024, rrad107
Research Square, 2024, 10.21203/rs.3.rs-3872267/v1
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.
Adv Sci (Weinh), 2023, 10(13):e2205436
Research Square, 2023, 10.21203/rs.3.rs-3629594/v1
J Cancer, 2022, 13(4):1203-1213
S2396 Salidroside Salidroside (Rhodioloside), a phenylpropanoid glycoside isolated from Rhodiola rosea, has been reported to have a broad spectrum of pharmacological properties.
Mol Med Rep, 2023, 27(2)37
Research Square, 2023, 10.21203/rs.3.rs-3696850/v1
FASEB J, 2021, 35(12):e22044
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.
S1847 Clemastine fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Neurobiol Dis, 2024, 190:106375
J Clin Invest, 2022, e152187
Front Pharmacol, 2022, 13:914153
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.
E0795 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. 

mTOR阻害剤の選択性比較

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