mTOR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

mTOR Products

All (57) mTOR Inhibitors (51) mTOR Activators (4) mTOR Modulators (2)

Catalog No.	Information	Product Use Citations	Product Validations
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 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Nat Microbiol, 2020, 10.1038/s41564-020-0782-1 Nat Commun, 2020, 14;11(1):1825 Genome Med, 2020, 18;12(1):17	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus, AY 22989, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.	Mol Med Rep, 2021, 23(1)9 Nature, 2020, 10.1038/s41586-020-2928-y Cell, 2020, 25;181(7):1596-1611.e27.	H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.
S1120	Everolimus (RAD001) Everolimus (RAD001) 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 Lett, 2021, 496:127-133 Cancer Cell, 2020, 37(2):183-199 Nat Commun, 2020, 26;11(1):2641	Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
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.	Nat Commun, 2020, 11(1):4684 Dev Cell, 2020, 55(3):298-313.e10 Clin Cancer Res, 2020, 10.1158/1078-0432	mTOR kinase inhibitor AZD8055 activates PI3K accompanied with induction of expression of EGFR, HER2, HER3 and IRS1. Serum-deprived CHO-EGFP-AKT cells were incubated with 50 nM AZD8055 for 24 hr. The EGFP signal was detected using confocal microscopy. The white arrows indicate EGFP-AKT located on cellular membrane.
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.	Proc Natl Acad Sci U S A, 2020, 117(49):31189-31197 Cancers (Basel), 2020, 17;12(1):232 Cell Oncol (Dordr), 2020, 8	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.
S3355^New	3-Hydroxyanthranilic acid 3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
S9611^New	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^New	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.
S6517^New	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.
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.	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485 Mol Ther Nucleic Acids, 2020, 1;20:801-811 Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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.	Nature, 2020, 10.1038/s41586-020-2960-y Blood, 2020, 5 pii: blood Adv Sci (Weinh), 2020, 7(20):2000157	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
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.	J Exp Clin Cancer Res, 2020, 39(1):38 Exp Cell Res, 2020, 15;388(2):111862 IUBMB Life, 2020, 10.1002/iub.2232	Effects of PI3K and mTOR inhibitors on IGF1R and AKT signaling in RMS cells. Rh41 cells were treated with 0.3 uM PI3K inhibitor BKM120, 0.3 uM mTOR inhibitor KU0063794 for the indicated time. Lysates were made and analyzed for p-AKT, S6RP and IGF1R.
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.	Sci Adv, 2020, 6(33):eabb8771 Mol Ther, 2020, 6;28(5):1339-1358 Mol Cancer Ther, 2020, 10.1158/1535-7163.MCT-19-1017	Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs^+24/44/ESA viability. CSCs^+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.
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.	PLoS Biol, 2019, 17(5):e3000252 Sci Signal, 2019, 12(589) Int J Mol Med, 2019, 43(1):47-56	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Neuro Oncol, 2020, 15;22(4):563-574	Hep-2 (D) or SCC-9 (E) cells were treated with PI3K/Akt and mTOR dual inhibitor LY 294002 (LY, 1 umol/L), mTORC1 inhibitor rapamycin (0.5 umol/L), mTORC1/2 dual inhibitor AZD2014 (0.1 uM), INK-128 (0.1 uM) or AZD8055 (0.1 uM) for 72 h, cell viability was analyzed. The mean of three independent experiments performed in triplicate was shown. Statistical significance was analyzed by ANOVA. p < 0.01 vs Control. *p < 0.01 vs. AZD8055 group.
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	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).
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.	Nature, 2020, 10.1038/s41586-020-03056-z Cell, 2020, S0092-8674(20)31627-5 Cell, 2020, 25;181(7):1596-1611.e27.	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.
S2658	Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with K_i 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.	Nat Commun, 2020, 11(1):71 Theranostics, 2020, 16;10(14):6483-6499 Cancer Res, 2020, canres.1992.2020
S2624	OSI-027 OSI-027 (ASP4786) 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.	Mol Ther Nucleic Acids, 2020, 1;20:801-811 Proc Natl Acad Sci U S A, 2019, 10.1073/pnas.1911393116 J Control Release, 2019, 317:67-77
S2743	PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i 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.	Ann Gastroenterol Surg, 2020, 4(5):571-579 Mol Cancer, 2019, Cancer Biol Med, 2019, 16(2):264-275	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.
S2696	Apitolisib (GDC-0980) 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 K_i 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.	J Clin Med, 2020, 9(12)E3878 Sci Rep, 2020, 10(1):16208 Cell Death Dis, 2019, 10(3):231	Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.
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.	BMC Cancer, 2020, 20(1):4 Cell Rep, 2019, 27(3):820-834 Biochem Pharmacol, 2019, 169:113640	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of GSK1059615 for 24 hours.
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.	Genome Med, 2020, 18;12(1):17 Cancer Biol Ther, 2020, Oncogene, 2019, 38(49):7433-7446	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.
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	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WYE-354 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
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.	Cancer Cell, 2020, 13;37(1):104-122e12 Nat Commun, 2020, 11(1):3258 Genome Med, 2020, 18;12(1):17
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.	Nature, 2020, 10.1038/s41586-020-2857-9 Nat Commun, 2020, 11(1):71 EMBO J, 2020, e104542	U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/P_i before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
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.	Oncotarget, 2017, 8(13):20974-20987 J Cell Sci, 2014, 127(Pt 4):788-800 PLoS One, 2014, 9(8):e105280	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.
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.	Cancer Biol Ther, 2017, 18(10):816-826 Oncotarget, 2016, 7(34):55690-55703 Oncotarget, 2016, 7(48):79842-79853	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).
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	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of Palomid529 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
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.	PLoS One, 2016, 11(10):e0164895 Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64	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.
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	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).
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 J, 2020, S2319-4170(20)30066-4 bioRxiv, 2020, 2020/9/20.4.7.30734 Nat Chem Biol, 2018, 14(1):94-101
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).	Front Cell Dev Biol, 2020, 8:383 Biochem Biophys Res Commun, 2016, 474(2):330-7	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).
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
S8040	GDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K_i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.	Cell Death Differ, 2020, 10.1038/s41418-020-00649-z Biochem Biophys Res Commun, 2016, 477(2):174-80	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.
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
S7369	4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with K_D of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.	Mol Pharmacol, 2021, 99(1):1-16 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Hep3B and PC3 cells were treated with 50 μmol/L 4EGI-1 or 5 μmol/L ABT alone or their combination for 48 hours, and then the cell viability was examined by CCK-8 assay. p, phosphorylated; t, total; T, Thr; S, Ser; , P < 0.05; , P < 0.01; **, P < 0.001.
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.
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.	Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
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.	Cells, 2020, 9(9)E2012 Cells, 2020, 9(9)E2110 J Pharmacol Exp Ther, 2019, 371(2):320-326
S7091	Zotarolimus (ABT-578) Zotarolimus (ABT-578) 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
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.
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.	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.	Oncol Rep, 2020, 43(3):773-782
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.	Genome Med, 2020, 18;12(1):17 Mol Cancer Ther, 2020, molcanther.1160.2019 Cell Oncol (Dordr), 2020, 8	HL60, HL60/ADR, K562 and K562/A02 cells pretreated with various concentrations of Voxtalisib (0, 0.625, 1.25, 2.5, 5 and 10 μM) for 48 h were harvested for western blot. The levels of cyclin D1, p27, and p-pRb in the nuclei were determined.
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	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
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	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".
S8322	Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.	Exp Ther Med, 2020, 20(4):3625-3632 Oncotarget, 2017, 8(58):98964-98973	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.
S6516	GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and K_iapp of 21 nM for mTOR.
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.	Biomed Res Int, 2020, 2020:4035306 J Neurosci, 2020, 40(29):5531-5548 Biomater Sci, 2019, 7(9):3779-3787
S7811	MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.	Theranostics, 2020, 16;10(14):6448-6466 J Exp Clin Cancer Res, 2020, 24;39(1):93 J Neuroinflammation, 2020, 17(1):329	Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; *P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; P < 0.05 vs. I+Exo-124 group.
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.	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.
S1847	Clemastine Fumarate Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.	Nat Neurosci, 2020, 10.1038/s41593-020-0588-8 Acta Neuropathol, 2020, 140(5):715-736 Anticancer Res, 2019, 39(7):3767-3775	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
S9514	Rotundic acid Rotundic 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.

Catalog No.	Information	Product Use Citations	Product Validations
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 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Nat Microbiol, 2020, 10.1038/s41564-020-0782-1 Nat Commun, 2020, 14;11(1):1825 Genome Med, 2020, 18;12(1):17	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1039	Rapamycin (Sirolimus) Rapamycin (Sirolimus, AY 22989, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.	Mol Med Rep, 2021, 23(1)9 Nature, 2020, 10.1038/s41586-020-2928-y Cell, 2020, 25;181(7):1596-1611.e27.	H4-LC3-GFP cells were treated with 1 nM IFNA2 for the indicated periods in the presence of 200 nM rapamycin. Images of the cells were collected using an ArrayScan HCS 4.0 Reader. Representative cells are shown. The average spot intensity in 500 cells from each indicated sample was determined. Data are displayed as means ?SD of the spot intensity per cell (below). RLU, relative leight unit.
S1120	Everolimus (RAD001) Everolimus (RAD001) 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 Lett, 2021, 496:127-133 Cancer Cell, 2020, 37(2):183-199 Nat Commun, 2020, 26;11(1):2641	Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 (2.5 uM), everolimus (1 uM), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
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.	Nat Commun, 2020, 11(1):4684 Dev Cell, 2020, 55(3):298-313.e10 Clin Cancer Res, 2020, 10.1158/1078-0432	mTOR kinase inhibitor AZD8055 activates PI3K accompanied with induction of expression of EGFR, HER2, HER3 and IRS1. Serum-deprived CHO-EGFP-AKT cells were incubated with 50 nM AZD8055 for 24 hr. The EGFP signal was detected using confocal microscopy. The white arrows indicate EGFP-AKT located on cellular membrane.
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.	Proc Natl Acad Sci U S A, 2020, 117(49):31189-31197 Cancers (Basel), 2020, 17;12(1):232 Cell Oncol (Dordr), 2020, 8	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.
S3355^New	3-Hydroxyanthranilic acid 3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
S9611^New	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^New	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.
S6517^New	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.
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.	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-2485 Mol Ther Nucleic Acids, 2020, 1;20:801-811 Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669	We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
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.	Nature, 2020, 10.1038/s41586-020-2960-y Blood, 2020, 5 pii: blood Adv Sci (Weinh), 2020, 7(20):2000157	Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6, fibrillarin, and tubulin were used as loading controls.Effects of DNAPK inhibitors on its autophosphorylation in bleomycin-treated cells.
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.	J Exp Clin Cancer Res, 2020, 39(1):38 Exp Cell Res, 2020, 15;388(2):111862 IUBMB Life, 2020, 10.1002/iub.2232	Effects of PI3K and mTOR inhibitors on IGF1R and AKT signaling in RMS cells. Rh41 cells were treated with 0.3 uM PI3K inhibitor BKM120, 0.3 uM mTOR inhibitor KU0063794 for the indicated time. Lysates were made and analyzed for p-AKT, S6RP and IGF1R.
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.	Sci Adv, 2020, 6(33):eabb8771 Mol Ther, 2020, 6;28(5):1339-1358 Mol Cancer Ther, 2020, 10.1158/1535-7163.MCT-19-1017	Synergistic effect of BMS-777607 with mTOR inhibitors in reduction of CSCs^+24/44/ESA viability. CSCs^+24/44/ESA at 5,000 cells per well with stem cell culture media in triplicate in an ultra-low adhesion plate were treated with 5 umol/L BMS-777607, 1 umol/L AZD8055, 1 umol/L RAD001, and 1 umol/L PP242 alone, or in their different combinations. Cells were cultured for 72 hours. Percentages of polyploid cells were determined by counting 300 cells from two different regions. Results shown here were from one of two experiments with similar results.
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.	PLoS Biol, 2019, 17(5):e3000252 Sci Signal, 2019, 12(589) Int J Mol Med, 2019, 43(1):47-56	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of Deforolimus for 24 hours.
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.	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Neuro Oncol, 2020, 15;22(4):563-574	Hep-2 (D) or SCC-9 (E) cells were treated with PI3K/Akt and mTOR dual inhibitor LY 294002 (LY, 1 umol/L), mTORC1 inhibitor rapamycin (0.5 umol/L), mTORC1/2 dual inhibitor AZD2014 (0.1 uM), INK-128 (0.1 uM) or AZD8055 (0.1 uM) for 72 h, cell viability was analyzed. The mean of three independent experiments performed in triplicate was shown. Statistical significance was analyzed by ANOVA. p < 0.01 vs Control. *p < 0.01 vs. AZD8055 group.
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	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).
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.	Nature, 2020, 10.1038/s41586-020-03056-z Cell, 2020, S0092-8674(20)31627-5 Cell, 2020, 25;181(7):1596-1611.e27.	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.
S2658	Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with K_i 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.	Nat Commun, 2020, 11(1):71 Theranostics, 2020, 16;10(14):6483-6499 Cancer Res, 2020, canres.1992.2020
S2624	OSI-027 OSI-027 (ASP4786) 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.	Mol Ther Nucleic Acids, 2020, 1;20:801-811 Proc Natl Acad Sci U S A, 2019, 10.1073/pnas.1911393116 J Control Release, 2019, 317:67-77
S2743	PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i 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.	Ann Gastroenterol Surg, 2020, 4(5):571-579 Mol Cancer, 2019, Cancer Biol Med, 2019, 16(2):264-275	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.
S2696	Apitolisib (GDC-0980) 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 K_i 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.	J Clin Med, 2020, 9(12)E3878 Sci Rep, 2020, 10(1):16208 Cell Death Dis, 2019, 10(3):231	Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.
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.	BMC Cancer, 2020, 20(1):4 Cell Rep, 2019, 27(3):820-834 Biochem Pharmacol, 2019, 169:113640	Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of GSK1059615 for 24 hours.
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.	Genome Med, 2020, 18;12(1):17 Cancer Biol Ther, 2020, Oncogene, 2019, 38(49):7433-7446	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.
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	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WYE-354 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
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.	Cancer Cell, 2020, 13;37(1):104-122e12 Nat Commun, 2020, 11(1):3258 Genome Med, 2020, 18;12(1):17
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.	Nature, 2020, 10.1038/s41586-020-2857-9 Nat Commun, 2020, 11(1):71 EMBO J, 2020, e104542	U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/P_i before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
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.	Oncotarget, 2017, 8(13):20974-20987 J Cell Sci, 2014, 127(Pt 4):788-800 PLoS One, 2014, 9(8):e105280	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.
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.	Cancer Biol Ther, 2017, 18(10):816-826 Oncotarget, 2016, 7(34):55690-55703 Oncotarget, 2016, 7(48):79842-79853	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).
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	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of Palomid529 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
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.	PLoS One, 2016, 11(10):e0164895 Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64	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.
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	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).
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 J, 2020, S2319-4170(20)30066-4 bioRxiv, 2020, 2020/9/20.4.7.30734 Nat Chem Biol, 2018, 14(1):94-101
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).	Front Cell Dev Biol, 2020, 8:383 Biochem Biophys Res Commun, 2016, 474(2):330-7	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).
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
S8040	GDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K_i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.	Cell Death Differ, 2020, 10.1038/s41418-020-00649-z Biochem Biophys Res Commun, 2016, 477(2):174-80	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.
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
S7369	4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with K_D of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.	Mol Pharmacol, 2021, 99(1):1-16 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Hep3B and PC3 cells were treated with 50 μmol/L 4EGI-1 or 5 μmol/L ABT alone or their combination for 48 hours, and then the cell viability was examined by CCK-8 assay. p, phosphorylated; t, total; T, Thr; S, Ser; , P < 0.05; , P < 0.01; **, P < 0.001.
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.
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.	Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
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.	Cells, 2020, 9(9)E2012 Cells, 2020, 9(9)E2110 J Pharmacol Exp Ther, 2019, 371(2):320-326
S7091	Zotarolimus (ABT-578) Zotarolimus (ABT-578) 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
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.
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.	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.	Oncol Rep, 2020, 43(3):773-782
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.	Genome Med, 2020, 18;12(1):17 Mol Cancer Ther, 2020, molcanther.1160.2019 Cell Oncol (Dordr), 2020, 8	HL60, HL60/ADR, K562 and K562/A02 cells pretreated with various concentrations of Voxtalisib (0, 0.625, 1.25, 2.5, 5 and 10 μM) for 48 h were harvested for western blot. The levels of cyclin D1, p27, and p-pRb in the nuclei were determined.
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	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
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	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".
S8322	Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.	Exp Ther Med, 2020, 20(4):3625-3632 Oncotarget, 2017, 8(58):98964-98973	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.
S6516	GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and K_iapp of 21 nM for mTOR.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Biomed Res Int, 2020, 2020:4035306 J Neurosci, 2020, 40(29):5531-5548 Biomater Sci, 2019, 7(9):3779-3787
S7811	MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.	Theranostics, 2020, 16;10(14):6448-6466 J Exp Clin Cancer Res, 2020, 24;39(1):93 J Neuroinflammation, 2020, 17(1):329	Exosomal miR-124-3p inhibited neuronal inflammation by suppressing the activity of mTOR signaling. A, B) Immunoblot (A) and quantitative (B) data of p-4E-BP1 and p-P70S6K in neurons after scratch injury and exosomal treatment. Their expression was increased after scratch injury and was suppressed by miR-124-3p–up-regulated exosomes, suggesting that miR-124-3p suppresses the activity of mTOR signaling (n = 6/group). ##P < 0.01 vs. control group; *P < 0.01 vs. injury group. C) Expression levels of inflammatory mediators in the culture medium were detected in the 3 groups of neurons: injured neurons (injury group), injured neurons treated with miR-124-3p–up-regulated exosomes (I+Exo-124), and injured neurons treated with miR-124-3p-up-regulated exosomes and the mTOR activator (MHY1485). Compared with the I+Exo-124 group, the MHY1485 group represented an increased expression on proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and a decreased expression of anti-inflammatory cytokines (IL-10), suggesting that MHY1485 blocks the anti-inflammatory effect of miR-124-3p in injured neurons. Thus, the inhibitory effect of exosomal miR-124-3p on neuronal inflammation was exerted by suppressing the activity of mTOR signaling (n = 6/group). #P < 0.05 vs. injury group; P < 0.05 vs. I+Exo-124 group.
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.	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.

Catalog No.	Information	Product Use Citations	Product Validations
S1847	Clemastine Fumarate Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.	Nat Neurosci, 2020, 10.1038/s41593-020-0588-8 Acta Neuropathol, 2020, 140(5):715-736 Anticancer Res, 2019, 39(7):3767-3775	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
S9514	Rotundic acid Rotundic 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.

Catalog No.

Information

Product Use Citations

Product Validations

S1847

Clemastine Fumarate

Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.

Nat Neurosci, 2020, 10.1038/s41593-020-0588-8

Acta Neuropathol, 2020, 140(5):715-736

Anticancer Res, 2019, 39(7):3767-3775

S9514

Rotundic 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.