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mTOR Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S1039 | Rapamycin (Sirolimus) | Rapamycin is a specific mTOR inhibitor with IC50 of ~0.1 nM in HEK293 cells. This compound binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. It is an autophagy activator and an immunosuppressant. |
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| S1120 | RAD001 (Everolimus) | Everolimus 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. |
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| 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. This compound induces caspase-dependent apoptosis and also induces autophagy. Phase 1. |
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| 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. |
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| 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. |
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| S2811 | Sapanisertib (MLN0128, INK-128) | 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. |
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| S1044 | Temsirolimus (CCI-779) | Temsirolimus is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis. |
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| S2218 | Torkinib (PP242) | Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; this compound targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. It induces mitophagy and apoptosis. |
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| S2783 | Vistusertib (AZD2014) | Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay, and is highly selective against multiple PI3K isoforms (α/β/γ/δ). It showed no or weak binding to the majority of kinases when tested at 1 μM. This compound induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity. |
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| 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. |
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| 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. This compound inhibits ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. It decreases cell viability and induces autophagy and apoptosis. |
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| 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. This compound induces autophagy in cancer cells. |
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| 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). |
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| S2661 | WYE-125132 (WYE-132) | WYE-125132 (WYE-132) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; it is highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR. |
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| S2238 | Palomid 529 (P529) | Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6. This compound is in Phase 1. |
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| 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. |
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| S7091 | Zotarolimus (ABT-578) | Zotarolimus (ABT-578, A 179578), an analogue of rapamycin, inhibits FKBP-12 binding with an IC50 of 2.8 nM. |
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| S2689 | WAY-600 | WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; this compound blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); it is selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold). |
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| 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. |
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| 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. |
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| S2668 | WYE-687 | WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; this compound 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). |
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| S8267 | RapaLink-1 | RapaLink-1, a third-generation bivalent inhibitor of mTOR, combines Rapamycin with MLN0128 using an inert chemical linker. It demonstrates efficacy against resistant mutants of malignant brain tumors and inhibits cancer cell progression by binding to mesenchymal markers. |
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| 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. |
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| S8298 | CZ415 | CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability. |
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| 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. | ||
| S8784 | PQR620 | PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. This compound has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure. | ||
| E5815 | YB-3-17 | YB-3−17 is a dual-target compound that effectively and selectively inhibits mTOR with an IC50 of 0.22 nM, while promoting GSPT1 degradation with an IC50 of 5 nM, leading to substantial tumor growth inhibition both in vitro and in vivo. It also exhibits significant antiproliferative activity in glioblastoma models. | ||
| S9883New | RMC-5552 | RMC-5552 is a selective bi-steric inhibitor of mTORC1, with the potential for treating mTORC1-activated tumors. It potently inhibits mTORC1-mediated phosphorylation of pS6K and p4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. | ||
| 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. | ||
| 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. It inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell, induces autophagy, and suppresses HIV-1 replication. Phase 2. |
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| S2638 | NU7441 (KU-57788) | NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM. It also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively, and reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage. |
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| 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. This compound induces apoptosis in murine T-cell Lymphoma. |
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| 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. This compound induces autophagy. Phase 1. |
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| 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. This compound induces apoptosis. Phase 2. |
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| S2298 | Fisetin | Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins. |
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| 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. It also acts as a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and is highly selective versus other PIKK family kinases. This compound activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2. |
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| S2628 | Gedatolisib (PKI-587) | Gedatolisib (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. This compound is currently in Phase 2. |
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| 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. |
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| 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). This compound modulates autophagy and inhibits mTORC1 signaling. |
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| 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. |
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| S7646 | Voxtalisib (XL765) | Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; this compound also inhibits DNA-PK and mTOR. Phase 1/2. |
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| 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. |
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| S8322 | Samotolisib (LY3023414) | Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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| 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. |
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| S8050 | ETP-46464 | ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S2406 | Chrysophanic Acid | Chrysophanic Acid (Chrysophanol) a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor. |
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| 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. |
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| S9736 | ME-344 | ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM. |
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| 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. |
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| 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. |
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| S5554 | Lanatoside C | Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. This compound induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways. | ||
| E2375 | PI3K/mTOR Inhibitor-2 | PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity. | ||
| 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. |
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