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PI3K/Akt/mTOR signaling mTOR

mTOR

The mammalian target of rapamycin (mTOR), sometimes also referred to as the mechanistic target of rapamycin and FK506-binding protein 12-rapamycin-associated protein 1 (FRAP1), is a kinase that in humans is encoded by the MTOR gene. mTOR is a member of the phosphatidylinositol 3-kinase-related kinase family of protein kinases.mTOR links with other proteins and serves as a core component of two distinct protein complexes, mTOR complex 1 and mTOR complex 2, which regulate different cellular processes. In particular, as a core component of both complexes, mTOR functions as a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription. As a core component of mTORC2, mTOR also functions as a tyrosine protein kinase that promotes the activation of insulin receptors and insulin-like growth factor 1 receptors. mTORC2 has also been implicated in the control and maintenance of the actin cytoskeleton.
Cat No. product name
T1537 RapamycinHOT Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
T1784 EverolimusHOT Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
T1838 INK 128 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...
T1859 AZD8055HOT 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.
T1861 Omipalisib GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
T1908 MHY1485 MHY1485 is a mTOR activator. It inhibits the autophagic process by inhibition of fusion between autophagosomes and lysosomes, leading to the accumulation of LC3...
T1916 Apitolisib 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...
T1958 AZ20 AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
T1961 Vistusertib AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
T1970 Gedatolisib 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.
T2083 PI3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
T2084 ETP46464 ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
T2144 TacrolimusHOT 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.
T2145 TemsirolimusHOT Temsirolimus is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
T2235 DactolisibHOT 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).
T2357 GSK-1059615 GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
T2414 TorkinibHOT Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
T2415 PP121 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) ,...
T2434 LY 303511 LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.
T2475 KU0063794 KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
T2616 PIK-93 PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
T2619 CH5132799 CH5132799 has been used in trials studying the treatment of Solid Tumors.
T2685 KU55933 KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T2706 Palomid 529 Palomid 529 has been used in trials studying the treatment of Age-Related Macular Degeneration.
T3153 Serabelisib MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
T3351 CC-223 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...
T3395 Timosaponin AIII Timosaponin AIII induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10μM). The Timosaponin AIII cellular response is mediated via inhibiti...
T3514 CZ415 CZ415 is a potent and highly selective mTOR inhibitor.
T3541 CC-115 CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
T3692 GNE 477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
T3705 GDC-0084 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...
T3986 SF2523 SF2523 is a highly selective and potent inhibitor.
T4199 Desmethyl-VS-5584 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.
T6030 XL388 XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
T6033 Zotarolimus Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
T6045 Torin 1 Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
T6100 Torin 2 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...
T6103 VS-5584 VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
T6319 OSI-027 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...
T6334 Ridaforolimus Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus bin...
T6510 GDC-0349 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...
T6731 WYE-354 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...
T6732 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...
T6883 LY3023414 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...
T4423 LY303511 hydrochloride LY303511 (NV-128)is a potent mTOR inhibitor
T4488 GSK-25 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...
T4639 MSDC 0602 MSDC-0602 is an insulin sensitizer potentially for the treatment of diabetes.
T1920 CapivasertibHOT 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).
T5338 mTOR inhibitor-1 C-4 is a potential ATP-competitive inhibitor of mTOR. C-4 could inhibit cell growth and proliferation.
T5472 PQR620 PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.
Rapamycin HOT
T1537CAS 53123-88-9
Rapamycin, a macrolide compound obtained from Streptomyces hygroscopicus, is a potent and specific mTOR inhibitor (IC50: 0.1 nM in HEK293 cells).
Everolimus HOT
T1784CAS 159351-69-6
Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.
INK 128
T1838CAS 1224844-38-5
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 HOT
T1859CAS 1009298-09-2
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.
Omipalisib
T1861CAS 1086062-66-9
GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
MHY1485
T1908CAS 326914-06-1
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
T1916CAS 1032754-93-0
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
T1958CAS 1233339-22-4
AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
Vistusertib
T1961CAS 1009298-59-2
AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
Gedatolisib
T1970CAS 1197160-78-3
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.
PI3065
T2083CAS 955977-50-1
PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
ETP46464
T2084CAS 1345675-02-6
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
Tacrolimus HOT
T2144CAS 104987-11-3
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 HOT
T2145CAS 162635-04-3
Temsirolimus is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
Dactolisib HOT
T2235CAS 915019-65-7
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).
GSK-1059615
T2357CAS 958852-01-2
GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
Torkinib HOT
T2414CAS 1092351-67-1
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
PP121
T2415CAS 1092788-83-4
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) ,...
LY 303511
T2434CAS 154447-38-8
LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.
KU0063794
T2475CAS 938440-64-3
KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2.
PIK-93
T2616CAS 593960-11-3
PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
CH5132799
T2619CAS 1007207-67-1
CH5132799 has been used in trials studying the treatment of Solid Tumors.
KU55933
T2685CAS 587871-26-9
KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
Palomid 529
T2706CAS 914913-88-5
Palomid 529 has been used in trials studying the treatment of Age-Related Macular Degeneration.
Serabelisib
T3153CAS 1268454-23-4
MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
CC-223
T3351CAS 1228013-30-6
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
T3395CAS 41059-79-4
Timosaponin AIII induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10μM). The Timosaponin AIII cellular response is mediated via inhibiti...
CZ415
T3514CAS 1429639-50-8
CZ415 is a potent and highly selective mTOR inhibitor.
CC-115
T3541CAS 1228013-15-7
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
GNE 477
T3692CAS 1032754-81-6
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
GDC-0084
T3705CAS 1382979-44-3
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
T3986CAS 1174428-47-7
SF2523 is a highly selective and potent inhibitor.
Desmethyl-VS-5584
T4199CAS 1246535-95-4
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
T6030CAS 1251156-08-7
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
T6033CAS 221877-54-9
Zotarolimus, an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).
Torin 1
T6045CAS 1222998-36-8
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
T6100CAS 1223001-51-1
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
T6103CAS 1246560-33-7
VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
OSI-027
T6319CAS 936890-98-1
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
T6334CAS 572924-54-0
Ridaforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus bin...
GDC-0349
T6510CAS 1207360-89-1
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
T6731CAS 1062169-56-5
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
T6732CAS 1062161-90-3
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
T6883CAS 1386874-06-1
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 hydrochloride
T4423CAS 2070014-90-1
LY303511 (NV-128)is a potent mTOR inhibitor
GSK-25
T4488CAS 874119-56-9
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
T4639CAS 1133819-87-0
MSDC-0602 is an insulin sensitizer potentially for the treatment of diabetes.
Capivasertib HOT
T1920CAS 1143532-39-1
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).
mTOR inhibitor-1
T5338CAS 468747-17-3
C-4 is a potential ATP-competitive inhibitor of mTOR. C-4 could inhibit cell growth and proliferation.
PQR620
T5472CAS 1927857-56-4
PQR620 is a novel potent and selective, brain penetrant inhibitor of mTORC1/2.