mTOR
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1009 | Dactolisib (BEZ235, NVP-BEZ235) | <1 mg/mL | 0.01 mg/mL | <1 mg/mL |
| S1039 | Rapamycin (Sirolimus) | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1120 | Everolimus (RAD001) | <1 mg/mL | 100 mg/mL | 7 mg/mL |
| S1555 | AZD8055 | <1 mg/mL | 50 mg/mL | 3 mg/mL |
| S1044 | Temsirolimus (CCI-779, NSC 683864) | <1 mg/mL | 67 mg/mL | 75 mg/mL |
| S8738 | Bimiralisib (PQR309) | <1 mg/mL | 6 mg/mL | <1 mg/mL |
| S1038 | PI-103 | <1 mg/mL | 24 mg/mL | <1 mg/mL |
| S1226 | KU-0063794 | <1 mg/mL | 16 mg/mL | <1 mg/mL |
| S2218 | Torkinib (PP242) | <1 mg/mL | 61 mg/mL | 18 mg/mL |
| S5003 | Tacrolimus (FK506) | <1 mg/mL | 94 mg/mL | 83 mg/mL |
| S1022 | Ridaforolimus (Deforolimus, MK-8669) | <1 mg/mL | 198 mg/mL | <1 mg/mL |
| S2811 | Sapanisertib (INK 128, MLN0128) | <1 mg/mL | 62 mg/mL | 2 mg/mL |
| S1523 | Voxtalisib (SAR245409, XL765) Analogue | <1 mg/mL | 12 mg/mL | <1 mg/mL |
| S2827 | Torin 1 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S2658 | Omipalisib (GSK2126458, GSK458) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2624 | OSI-027 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
| S2743 | PF-04691502 | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S2696 | Apitolisib (GDC-0980, RG7422) | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S1360 | GSK1059615 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S2628 | Gedatolisib (PF-05212384, PKI-587) | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S1266 | WYE-354 | <1 mg/mL | 99 mg/mL | <1 mg/mL |
| S2783 | Vistusertib (AZD2014) | <1 mg/mL | 38 mg/mL | <1 mg/mL |
| S2817 | Torin 2 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S2661 | WYE-125132 (WYE-132) | <1 mg/mL | 104 mg/mL | <1 mg/mL |
| S2749 | BGT226 (NVP-BGT226) | <1 mg/mL | 30 mg/mL | <1 mg/mL |
| S2238 | Palomid 529 (P529) | <1 mg/mL | 81 mg/mL | <1 mg/mL |
| S2622 | PP121 | <1 mg/mL | 64 mg/mL | 2 mg/mL |
| S2668 | WYE-687 | <1 mg/mL | 0.5 mg/mL | <1 mg/mL |
| S2689 | WAY-600 | <1 mg/mL | 22 mg/mL | 2 mg/mL |
| S8050 | ETP-46464 | <1 mg/mL | 6 mg/mL | <1 mg/mL |
| S8040 | GDC-0349 | <1 mg/mL | 91 mg/mL | 6 mg/mL |
| S7035 | XL388 | <1 mg/mL | 23 mg/mL | <1 mg/mL |
| S7891 | CC-115 | <1 mg/mL | 67 mg/mL | <1 mg/mL |
| S7091 | Zotarolimus(ABT-578) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8163 | GDC-0084 | <1 mg/mL | 8 mg/mL | <1 mg/mL |
| S8298 | CZ415 | <1 mg/mL | 91 mg/mL | <1 mg/mL |
| S8589 | SF2523 | <1 mg/mL | 29 mg/mL | 7 mg/mL |
| S7646 | Voxtalisib (XL765, SAR245409) | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S2406 | Chrysophanic Acid | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S7886 | CC-223 | <1 mg/mL | 79 mg/mL | 79 mg/mL |
| S8322 | LY3023414 | <1 mg/mL | 47 mg/mL | 61 mg/mL |
| S8317 | 3BDO | <1 mg/mL | 65 mg/mL | 49 mg/mL |
| S7811 | MHY1485 | <1 mg/mL | 4 mg/mL | <1 mg/mL |
Isoform-specific Inhibitors
- mTOR Inhibitors (43)
- New mTOR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1009 |
Dactolisib (BEZ235, NVP-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. |
Level of phospho-proteins in RTK and PI3K–Akt–mTOR pathways in treated tumours, detected with western blot.
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| S1039 |
Rapamycin (Sirolimus)Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells. |
Protein blots showing MYC expression in naive and persister cells after 3 d of treatment with 2 uM AKT inhibitor MK-2206 (AKTi) or 10 nM mTOR inhibitor rapamycin (Rapa). |
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| S1120 |
Everolimus (RAD001)Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. |
Effects on PI3K signaling. Tumor cells were treated with DMSO, BEZ-235 (5uM, 1uM), BKM-120 (5uM, 1uM), RAD-001(5uM, 1uM) or cyclopamine (2.5uM, 1uM) for 3 hr. Cells were lysed and protein was analyzed for phosphorylation of AKT and S6 (pAKT and pS6) or for GAPDH by Western blotting.
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| S1555 |
AZD8055AZD8055 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. Phase 1. |
PC3-LN4 cells were treated with GSK690693 (5 uM) alone, or in combination with PP242 (2 uM) or AZD8055 (1 uM) for 24 h, and immunoblotting performed.
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| S1044 |
Temsirolimus (CCI-779, NSC 683864)Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. |
mTOR inhibitors attenuate ganetespib-driven elevation of HSPs in multiple tumor cell types. A375 melanoma cells were treated with vehicle, ganetespib (25 nmol/L), BEZ235 (500 nmol/L), or temsirolimus (500 nmol/L), either alone or in combination, for 24 hours. The levels of HSP90α, HSP70, HSP27, and GAPDH were determined by immunoblotting.
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| S8738New |
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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| S1038 |
PI-103PI-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. |
(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
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| S1226 |
KU-0063794KU-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. |
mTORC2-mediated stretch-induced SGK-1 phosphorylation. SMCs infected with Ad-SGK-1 were pretreated with PPP (10 μmol/L), rapamycin (100 nmol/L),or Ku-0063794 (10 μmol/L) for 30 minutes and then were subjected to stretch or IGF-1 (10 ng/mL) for 30 minutes.
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| 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. |
MTORC1 regulates the subcellular distribution of TFEB. Immunofluorescence confocal microscopy showing nuclear localization of recombinant TFEB-Flag in ARPE-19 cells incubated with MTORC1 inhibitors (PP242, LY294002, Wortmannin).
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| S5003 |
Tacrolimus (FK506)Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. |
Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry. |
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| S1022 |
Ridaforolimus (Deforolimus, MK-8669)Ridaforolimus (Deforolimus, MK-8669) 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. |
Protein analysis of ARK1 and ARK2 (A) xenografts following acute therapy with vehicle, ridaforolimus, lapatinib and trastuzumab or the triple combination.
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| S2811 |
Sapanisertib (INK 128, MLN0128)Sapanisertib (INK 128, MLN0128) 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. |
Blockade of PD-1 in combination with INK128 inhibits liver cancer cell proliferation and clone formation in vitro in immunocompetent mice. (A) Representative pictures show the clone formation of different administered groups in SMMC7721 PD-1 OE cells. (B) Histogram showing mean number of cloned formed 6 SD in each group. P < 0.05. (C) Optical density values 6 SD of Cell Counting Kit 8 assay in different administered groups in SMMC7721 PD-1 OE cells. (D,E) Flow-cytometric assessment of cell death with percent of annexin V1/7-aminoactinomycin D1 cells, mean 6 SEM. (F,G) Tumor growth kinetics (mean±SD) of different administered groups versus corresponding control in C57BL/6 mice subcutaneously implanted with PD-1 OE or vector-control Hepa1-6 cells. *P < 0.5; **P < 0.01; ***P < 0.001; #, not significant. Abbreviations: 7-AAD, 7-aminoactinomycin D; CCK8, Cell Counting Kit 8; NS, not significant; OD, optical density.
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| S1523 |
Voxtalisib (SAR245409, XL765) AnalogueVoxtalisib (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. |
The TMZ/XL765 combination decreases serum GH and PRL of mice bearing GH3 xenografts. A and B, After treatment with DMSO, TMZ, XL765, or the XL765/TMZ combination, the blood of the nude mice xenograft with GH3 tumor was collected and serum rat-GH and rat-PRL were measured by IRMA (TMZ/XL765 combination vs TMZ or XL765 alone: ***P <.001). |
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| S2827 |
Torin 1Torin 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. |
Huh-7.5 cells were treated with increasing concentration of Torin 1, a known autophagy inducer, and the autophagy response was assessed by measuring LC3II and p62 levels.
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| S2658 |
Omipalisib (GSK2126458, GSK458)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. Phase 1. |
Cells from C76N treated with indicated doses of omipalisib (GSK2126458) were lysed and electrophoresced through a 4-15% gradient gel and immunoblotted using the indicated antibodies. Dose-dependent increase in LC3 A and B (lower band) is noted.
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| S2624 |
OSI-027OSI-027 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. Phase 1. |
Cells were treated during 7 days with OSI-027 (C, D). Response is expressed as the percentage of vehicle-treated control (±s.e.m.). Control is normalised at 100%.
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| S2743 |
PF-04691502PF-04691502 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. Phase 2. |
BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
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| S2696 |
Apitolisib (GDC-0980, RG7422)Apitolisib (GDC-0980, RG7422) 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. Phase 2. |
Inhibition of PI3Kγ or PI3Kδ significantly decreased the migration of JVM3 cells. JVM3 cells were cultured in medium or stimulated for 24 h with CD40L/IL-4 and then incubated with the PI3Kγ-specific inhibitor CZC24832 (2 µM), the PI3Kδ-specific inhibitor idelalisib (1 µM), dual PI3Kδ/γ inhibitor duvelisib (1 µM), or the pan-PI3K inhibitor GDC0980 (1 µM) and subjected to a transwell migration assay. DMSO served as the vehicle control for the inhibitors, while SDF1α (100 ng/ml) served as the chemoattractant (n = 7).
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| S1360 |
GSK1059615GSK1059615 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. |
The PI3K/AKT pathway significantly contributes to the ligand-driven HER2 signaling activities detected by CELx HSF tests. a and b SKBr3 cells were seeded in sensor plates and then treated with a serial titration of the PI3K/AKT pathway inhibitor GSK1059615 (0 nM to 810 nM) two hours prior to maximal stimulation with NRG1b (800 pM) (a) or EGF (600 pM) (b). CELx curves are displayed using Delta CI values to demonstrate the relative signals to the time point (arrow) when the stimulus (EGF or NRG1b) was added. Dose–response curves of GSK1059615 inhibition on NRG1b and EGF-driven HER2 signals are shown in the insets
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| S2628 |
Gedatolisib (PF-05212384, 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. |
PI3K inhibitors promote apoptosis in checkpoint-defective cell lines. Two checkpoint-functional (A2058, D28) and three defective (HT144, D20, SKMel13) melanoma cell lines growth as tumour spheres as in Figure 4B were either untreated or treated with 5 uM PF-05212384 for 72 h, harvested and immunoblotted for pAkt Ser473.
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| S1266 |
WYE-354WYE-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). |
MTOR Inhibitor WYE-354 Had Anti-tumor Activity Comparable to that of miR-199a-3p. The histological evaluation of liver lesions showed a similar reduction in number and size of tumor nodules in mice treated with both miR-199a-3p and the MTOR inhibitor. In the figure, miR-199a-3p is indicated as miR-199.
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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; 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. |
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| S2817 |
Torin 2Torin 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. |
Immunofluorescent imaging of HAECs using VE-CAD (red) and p120 (green) antibodies was performed 12 h after DMSO (control), Torin-2 (100 nM), or EVL (500 nM) treatments. White arrows denote interendothelial gaps. White bar indicates 50 μm. EVL treatment increased VE-CAD mobilization from the membrane into the cytosol (relative to DMSO) with evidence of intracellular deposits and interendothelial gaps, whereas in DMSO-treated cells, there was colocalization of p120 and VE-CAD (yellow border) with no evidence of gap formation. In Torin-2-treated cells, there was evidence of colocalization of p120 and VE-CAD at cell borders with minimal interendothelial gap formation.
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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; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR. |
SW620 and SW620:8055R cells were treated with increasing concentrations of WYE-125132 for 24 hours and cell proliferation was assayed by [3H]thymidine incorporation. Results are the mean盋oV for three biological replicates from a single experiment; identical results were obtained in n=3 experiments.
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| S2749 |
BGT226 (NVP-BGT226)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. |
IGROV1-R10 cells were treated with BGT266(250nM) for 8 h.The effect of BGT226 on PI3K/Akt/mTOR pathway activation (A) and on expression of Mcl-1 and Bim (B). |
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| S2238 |
Palomid 529 (P529)Palomid 529 (P529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS6 but no effect observed on pMAPK or pAktT308. Phase 1. |
(A) Cell growth rate fromP529 (2 μM) and vehicle treated MFN2 knockout MCF-7 (left) and A549 cells (right). (B) Representative pictures (left) and statistical analysis (right) shown colony formation from P529 and vehicle treated MFN2 knockout MCF-7 and A549 cells. (C,D) In vitro wound closure of P529 and vehicle treated MFN-2 knockout MCF-7 cells (C) and A549 cells (D) from 24 h after scratch assay.
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| S2622 |
PP121PP-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. |
PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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| S2668 |
WYE-687WYE-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). |
Immunofluorescent double staining for K19 and pHH3 on HepG2 cells in non-coated condition, Ln-332 coated condition or Ln-332 coated condition supplemented with mTOR inhibitors (either rapamycin or WYE-687; n = 4). |
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| S2689 |
WAY-600WAY-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). |
WAY-600 blocks mTORC1/2 activation, but activates MEK-ERK signaling in HCC cells. HepG2 cells or primary HCC cells (“Pnt-2”) were treated with WAY-600 (“WAY”, 100 nM) for 1 h, mTOR-Raptor-Rictor association was tested by co-immunoprecipitation assay (A, for HepG2 cells), expression of listed kinases (p- and regular) was tested by Western blots (BeE).
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| S8050 |
ETP-46464ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
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| S8040 |
GDC-0349GDC-0349 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. |
The established (SQ20B/UMSCC47/SCC90 cells) or primary (“P1/P2/P3”) human NSCC cells as well as normal oral epithelial cells (“Epithelial cells”) were treated with indicated concentration of
GDC-0349, rapamycin (“Rap”) or RAD001 for applied time, cell proliferation was tested by CCK-8 assay. Expression of listed proteins in primary human NSCC cells was tested by Western blot analysis (D, right panel). “UNTR” indicates untreated control cells. * p < 0.05 vs. “UNTR” cells. # p < 0.05 vs. GDC-0349-only cells.
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| S7035 |
XL388XL388 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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| S7891 |
CC-115CC-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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| S7091 |
Zotarolimus(ABT-578)Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM. |
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| S8163 |
GDC-0084GDC-0084 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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| S8298 |
CZ415CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability. |
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| S8589 |
SF2523SF2523 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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| S7646 |
Voxtalisib (XL765, SAR245409)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. |
Cell viability measurements. The IMR-32, LA-N-1 and CHP‑134 cells were treated with mTOR/PI3K inhibitor SAR245409 alone or in combination with the 14G2a mAb (40 μg/ml) for 72 h. The cell viability was
determined by measuring ATP content, and compared to respective controls treated with appropriate diluents (DMSO or water, set as 1). P-values for t-test were as follows: *p<0.05, **p<0.01, ***p<0.001.
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| S2406 |
Chrysophanic AcidChrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor. |
After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of Chrysophanic acid for 3h,followed by 15-minute stimolation of 100ng/ml EGF |
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| S7886 |
CC-223CC-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. |
Fig 1. CC-223 is cytotoxic and anti-proliferative to cultured human HCC cells. Cultured HCC cell lines (HepG2, KYN-2 and Huh-7 lines), L02 normal hepatocytes as well as the primary human HCC cells ("HCC1/2/3" lines) were either left untreated ("C", same for all figures) or treated with designated concentration of CC-223 (10–1000 nM), cells were further cultivated in conditional medium for indicated time; Cell survival (A, B, C and E), and proliferation (D) were tested by listed assays. Data were expressed as mean ± SD (Same for all figures). n = 5 means five replicate wells (Same for Figs 1–4). * p <0.05 vs. "C".
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| S8322 |
LY3023414LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
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| S8317 |
3BDO3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. |
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| S7811 |
MHY1485MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy. |
MYH1485, an activator of mTOR, reduced LC3II production and inhibited autophagosome formation in PAR2-knockdown cells.
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