||Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
||Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
||INK 128 is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
||AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
||GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
||MHY1485 is a mTOR activator. It inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes, leading to the accumulation of LC3II protein and enlar
||Apitolisib, an effective, class I PI3K inhibitor for PI3Kα（IC50=5 nM）, PI3Kβ（IC50=27 nM）, PI3Kδ（IC50=7 nM）, PI3Kγ （IC50=14 nM）, is used in trials study of solid
||AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
||AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
||Gedatolisib is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
||PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
||ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
||Tacrolimus can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
||Temsirolimus is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
||Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
||GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
||Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
||PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-P
||LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.
||KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
||PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
||CH5132799 has been used in trials studying the treatment of Solid Tumors.
||KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
||Palomid 529 has been used in trials studying the treatment of Age-Related Macular Degeneration.
||MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
||CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and
||Timosaponin AIII induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10μM). The Timosaponin AIII cellular response is mediated via inhibition of mTORC1 and ind
||CZ415 is a potent and highly selective mTOR inhibitor.
||CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
||GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
||GDC-0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC-0084 specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, th
||SF2523 is a highly selective and potent inhibitor.
||Desmethyl-VS-5584 is a dimethyl analog of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
||XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
||Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
||Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
||Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of To
||VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
||OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ
||Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits t
||GDC-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.
||WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2/P-AKT(S473) and mTORC1/P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is
||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
||LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neoplasm, Solid Tumor, CO
||LY303511 (NV-128)is a potent mTOR inhibitor
||GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (
||MSDC-0602 is an insulin sensitizer potentially for the treatment of diabetes.
||Capivasertib (AZD5363) is a new-type orally available inhibitor of the serine/threonine protein kinase AKT (IC50s: 3/7/7 nM for Akt1/2/3).
||C-4 is a potential ATP-competitive inhibitor of mTOR. C-4 could inhibit cell growth and proliferation.
||PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.
||GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3
||PI3K-IN-2 is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta
||PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).
||Dihydromyricetin is a natural antioxidant flavonoid from Ampelopsis grossedentata. Dihydromyricetin is a potent inhibitor of dihydropyrimidinase with an IC50 of 48 μM. Dihydromyri
||3-Deoxysappanchalcone is an effective HO-1 inducer at the translational level.
||Onjisaponin B induces autophagy via the AMPK-mTOR signaling pathway, increases the NGF level and accelerates both the removal of mutant huntingtin and A53T α±-synuclein, it may h
||Pulsatilla saponin D
||Pulsatilla saponin D exhibits anticancer activities in various cancer types, it Inhibits autophagic flux and synergistically enhances the anticancer activity of chemotherapeutic ag
||(-)-Syringaresinol may be a potential chemotherapeutic agent for the treatment of cancer; it against H/R-induced cardiomyocyte injury and death, the degradation of HIF-1α± throug
||Zeylenone has good antitumor efficacy, it inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways. Zeylenone shows inhibito
||mTOR inhibitor-3 is an inhibitor of remarkably selective mTOR (Ki : 1.5 nM)
||mTOR inhibitor-2 is an inhibitor of selective and oral mTOR (IC50 of 7 nM).
||NV-5138 is a selective and orally active activator of brain mTORC1, with antidepressant effects.
||3BDO is an activator of mTOR. It can also inhibit autophagy..
||Dactolisib Tosylate (BEZ235 Tosylate) is an inhibitor of dual PI3K and mTOR kinase(IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively). Dactolisib Tosylate also inh
||FT-1518 ,exhibits antitumor activity, is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor.
||K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
||N6-Cyclopentyladenosine (CPA) is a selective agonist of Adenosine A1 receptor (Ki: 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively).
||DMH25 is a novel covalent and potent inhibitor of mTOR and shows in vivo antitumor activity against triple-negative breast cancer cells.
||Jolkinolide B has potent anti-inflammatory, and antitumor activities, it is able to enhance apoptosis of human leukemic HL-60 and THP-1 cells, at least in part, through downregulat
||Vicenin -2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen
||Vincristine-induced nociceptive painful sensation, may be due to its potential of antioxidative, neuroprotective and calcium channel inhibitory action.Vincristine can treat MM, ERK
||7-(4-Hydroxyphenyl)-1-phenyl-4-hepten-3-one as a beneficial compound to ameliorate the deleterious effects of Aβ on dendrite integrity and cell survival, and may provide new insig
||1,4-O-Diferuloylsecoisolariciresinol(9,9'-Di-O-(E)-feruloylsecoisolariciresinol),and pierreione B, two novel inhibitors of mTOR signaling, have strong anticancer activity. (+)-9,9'
||Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid peroxidation.Hirsutenon
||Jolkinolide A has anti-tumor activity. It inhibited VEGF expression in A549 cells through the inhibition of the Akt-STAT3-mTOR signaling pathway, and directly inhibited the prolife
||Kazinol A shows strong inhibition of arachidonic acid (AA)-induced platelet aggregation. It also exhibits potent inhibition with IC50 values ranging 0.6-164 M against XOD. Kazinol
||Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity.
||Sprengerinin C exerts anti-tumorigenic effects in hepatocellular carcinoma via inhibition of proliferation and angiogenesis and induction of apoptosis, it can strongly suppress tum
||Tomatidine shows antibiotic, and anti-inflammatory activities, it significantly suppresses the activity of ACAT and leads to reduction of atherogenesis. Tomatidine inhibits the inv
||TMBIM6 antagonist-1 is an antagonist of TMBIM6.