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 activ...
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 LC3...
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 t...
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) ,...
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...
Timosaponin AIII induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10μM). The Timosaponin AIII cellular response is mediated via inhibiti...
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) s...
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 proper...
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 PI...
Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus bin...
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 sele...
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...
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 Neopl...
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 imp...
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. |