1. Signaling Pathways
  2. PI3K/Akt/mTOR
  3. mTOR

mTOR

mTOR

Mammalian target of Rapamycin

mTOR (mammalian target of Rapamycin) is a protein that in humans is encoded by the mTOR gene. mTOR is a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, and transcription. mTOR belongs to the phosphatidylinositol 3-kinase-related kinase protein family. mTOR integrates the input from upstream pathways, including growth factors and amino acids. mTOR also senses cellular nutrient, oxygen, and energy levels. The mTOR pathway is dysregulated in human diseases, such as diabetes, obesity, depression, and certain cancers. Rapamycin inhibits mTOR by associating with its intracellular receptor FKBP12. The FKBP12-rapamycin complex binds directly to the FKBP12-Rapamycin Binding (FRB) domain of mTOR, inhibiting its activity.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114267
    Cbz-B3A
    Inhibitor ≥98.0%
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
    Cbz-B3A
  • HY-B1787
    Sulindac sulfone
    Inhibitor 98.10%
    Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research.
    Sulindac sulfone
  • HY-17471AR
    Metformin (hydrochloride) (Standard)
    Inhibitor 99.97%
    Metformin hydrochloride (Standard) is the analytical standard of Metformin (hydrochloride). This product is intended for research and analytical applications. Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
    Metformin (hydrochloride) (Standard)
  • HY-N2303
    Eriocalyxin B
    Inhibitor 99.93%
    Eriocalyxin B is a diterpenoid compound that can be isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B exhibits multiple activities, such as anti-cancer, anti-inflammatory, and inhibition of adipogenesis. Eriocalyxin B is capable of inducing apoptosis and autophagy in tumor cells. Eriocalyxin B can be used in the research of cancers, autoimmune diseases, and other conditions.
    Eriocalyxin B
  • HY-N0486R
    L-Leucine (Standard)
    Activator
    L-Leucine (Standard) is the analytical standard of L-Leucine. This product is intended for research and analytical applications. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
    L-Leucine (Standard)
  • HY-111065
    OXA-01
    Inhibitor
    OXA-01 is a potent mTORC1 and mTORC2 inhibitor, with IC50 values of 29 nM and 7 nM, respectively.
    OXA-01
  • HY-10218S
    Everolimus-d4
    Inhibitor
    Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
    Everolimus-d<sub>4</sub>
  • HY-147284
    PI3K-IN-37
    Inhibitor ≥99.0%
    PI3K-IN-37 (Example 84.1) is a PI3K α/β/δ inhibitor with IC50s of 6, 8, 4 nM, respectively. PI3K-IN-37 can also inhibit mTOR (IC50=4 nM).
    PI3K-IN-37
  • HY-N4315
    Pomiferin
    Inhibitor 98.98%
    Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
    Pomiferin
  • HY-10620
    PI3K-IN-22
    Inhibitor 99.50%
    PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer.
    PI3K-IN-22
  • HY-N6996R
    Methyl Eugenol (Standard)
    Inhibitor
    Methyl Eugenol (Standard) is the analytical standard of Methyl Eugenol. This product is intended for research and analytical applications. Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury.
    Methyl Eugenol (Standard)
  • HY-15271A
    WYE-687 dihydrochloride
    Inhibitor ≥98.0%
    WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
    WYE-687 dihydrochloride
  • HY-156027
    SIRT6-IN-3
    Inhibitor 98.19%
    SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC50=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.
    SIRT6-IN-3
  • HY-N3628
    Coronarin A
    Inhibitor ≥98.0%
    Coronarin A is an orally active natural compound that inhibits mTORC1 and S6K1 to increase IRS1 activity. Coronarin A shows anti-inflammatory activity and can also be used for type 2 diabetes mellitus research.
    Coronarin A
  • HY-109633
    PI3K-IN-18
    Inhibitor ≥99.0%
    PI3K-IN-18 (Compound 1) is a PI3K inhibitor, and can also effectively inhibit the homologous enzymemTOR. The IC50 values of PI3K-IN-18 for mTOR and PI3K-α were 49 nM and 41 nM, respectively.
    PI3K-IN-18
  • HY-N5136
    25(R,S)-Ruscogenin
    Inhibitor 99.83%
    Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway. And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
    25(R,S)-Ruscogenin
  • HY-P3072
    Mastoparan 17
    Control 98.15%
    Mastoparan 17 is a tetradecapeptide. Mastoparan 17 is an inactive analogue of Mastoparan (HY-P0246) .
    Mastoparan 17
  • HY-155066
    FD274
    Inhibitor 99.45%
    FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research.
    FD274
  • HY-N0486S12
    L-Leucine-d2
    Activator ≥99.0%
    L-Leucine-d2 is the deuterium labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway[1].
    L-Leucine-d<sub>2</sub>
  • HY-157169
    IBL-302
    Inhibitor 98.21%
    IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629).
    IBL-302
Cat. No. Product Name / Synonyms Application Reactivity

The mammalian target of rapamycin (mTOR) signaling pathway integrates both intracellular and extracellular signals and serves as a central regulator of cell metabolism, growth, proliferation and survival[1]. mTOR is the catalytic subunit of two distinct complexes called mTORC1 and mTORC2. mTORC1 comprises DEPTOR, PRAS40, RAPTOR, mLST8, mTOR, whereas mTORC2 comprises DEPTOR, mLST8, PROTOR, RICTOR, mSIN1, mTOR[2]. Rapamycin binds to FKBP12 and inhibits mTORC1 by disrupting the interaction between mTOR and RAPTOR. mTORC1 negatively regulates autophagy through multiple inputs, including inhibitory phosphorylation of ULK1 and TFEB. mTORC1 promotes protein synthesis through activation of the translation initiation promoter S6K and through inhibition of the inhibitory mRNA cap binding 4E-BP1, and regulates glycolysis through HIF-1α. It promotes de novo lipid synthesis through the SREBP transcription factors. mTORC2 inhibits FOXO1,3 through SGK and Akt, which can lead to increased longevity. The complex also regulates actin cytoskeleton assembly through PKC and Rho kinase[3]

 

Growth factors: Growth factors can signal to mTORC1 through both PI3K-Akt and Ras-Raf-MEK-ERK axis. For example, ERK and RSK phosphorylate TSC2, and inhibit it.

 

Insulin Receptor: The activated insulin receptor recruits intracellular adaptor protein IRS1. Phosphorylation of these proteins on tyrosine residues by the insulin receptor initiates the recruitment and activation of PI3K. PIP3 acts as a second messenger which promotes the phosphorylation of Akt and triggers the Akt-dependent multisite phosphorylation of TSC2. TSC is a heterotrimeric complex comprised of TSC1, TSC2, and TBC1D7, and functions as a GTPase activating protein (GAP) for the small GTPase Rheb, which directly binds and activates mTORC1. mTORC2 primarily functions as an effector of insulin/PI3K signaling. 

 

Wnt: The Wnt pathway activates mTORC1. Glycogen synthase kinase 3β (GSK-3β) acts as a negative regulator of mTORC1 by phosphorylating TSC2. mTORC2 is activated by Wnt in a manner dependent on the small GTPase RAC1[4].

 

Amino acids: mTORC1 senses both lysosomal and cytosolic amino acids through distinct mechanisms. Amino acids induce the movement of mTORC1 to lysosomal membranes, where the Rag proteins reside. A complex named Ragulator, interact with the Rag GTPases, recruits them to lysosomes through a mechanism dependent on the lysosomal v-ATPase, and is essential for mTORC1 activation. In turn, lysosomal recruitment enables mTORC1 to interact with GTP-bound RHEB, the end point of growth factor. Cytosolic leucine and arginine signal to mTORC1 through a distinct pathway comprised of the GATOR1 and GATOR2 complexes.    

 

Stresses: mTORC1 responds to intracellular and environmental stresses that are incompatible with growth such as low ATP levels, hypoxia, or DNA damage. A reduction in cellular energy charge, for example during glucose deprivation, activates the stress responsive metabolic regulator AMPK, which inhibits mTORC1 both indirectly, through phosphorylation and activation of TSC2, as well as directly through the phosphorylation of RAPTOR. Sestrin1/2 are two transcriptional targets of p53 that are implicated in the DNA damage response, and they potently activate AMPK, thus mediating the p53-dependent suppression of mTOR activity upon DNA damage. During hypoxia, mitochondrial respiration is impaired, leading to low ATP levels and activation of AMPK. Hypoxia also affects mTORC1 in AMPK-independent ways by inducing the expression of REDD1, the protein products of which then suppress mTORC1 by promoting the assembly of TSC1-TSC2[2].

 

Reference:

[1]. Laplante M, et al.mTOR signaling at a glance.J Cell Sci. 2009 Oct 15;122(Pt 20):3589-94. 
[2]. Zoncu R, et al. mTOR: from growth signal integration to cancer, diabetes and ageing.Nat Rev Mol Cell Biol. 2011 Jan;12(1):21-35. 
[3]. Johnson SC, et al. mTOR is a key modulator of ageing and age-related disease.Nature. 2013 Jan 17;493(7432):338-45.
[4]. Shimobayashi M, et al. Making new contacts: the mTOR network in metabolism and signalling crosstalk.Nat Rev Mol Cell Biol. 2014 Mar;15(3):155-62.

mTOR

mTORC1

mTORC2

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mTOR Inhibitors, Activators & Modulators
Product NamemTORmTORC1mTORC2Purity    
Rapamycin 
mTOR, IC50: 0.1 nM (in HEK293 cells )
 99.94%
MHY1485 
mTORC1
mTORC2
99.93%
Everolimus 
mTOR, IC50: 5-6 nM
 99.85%
Torin 1
mTOR, IC50: 3 nM
mTORC1, IC50: 2-10 nM
mTORC2, IC50: 2-10 nM
99.28%
AZD-8055
mTOR, IC50: 0.8 nM
  99.60%
Sapanisertib
mTOR, IC50: 1 nM
  99.66%
Salidroside
mTOR
  99.90%
Temsirolimus 
mTOR, IC50: 1.76 μM
 99.56%
L-Leucine 
mTORC1
 99.79%
Dactolisib
mTOR, IC50: 20.7 nM
  99.94%
Torin 2
mTOR, IC50: 2.81 nM
mTOR, EC50: 0.25 nM (Cell Assay)
  99.65%
PI-103 
mTORC1, IC50: 20 nM
mTORC2, IC50: 83 nM
99.82%
RMC-5552 
mTORC1
 98.10%
Omipalisib 
mTORC1, Ki: 0.18 nM
mTORC2, Ki: 0.3 nM
99.94%
Camonsertib
mTOR, IC50: 120 nM
  99.75%
RapaLink-1
mTOR
  99.92%
3BDO
mTOR
  99.93%
JR-AB2-011  
mTORC2, IC50: 0.36 μM
98.15%
Dihydromyricetin 
mTORC1
mTORC2
99.73%
Torkinib
mTOR, IC50: 8 nM
mTORC1, IC50: 30 nM
mTORC2, IC50: 58 nM
99.03%
Aloe emodin  
mTORC2
98.32%
hSMG-1 inhibitor 11j
mTOR, IC50: 50 nM
  99.82%
Vistusertib
mTOR, IC50: 2.81 nM
  99.32%
KU-0063794 
mTORC1, IC50: 10 nM
mTORC2, IC50: 10 nM
99.67%
Gedatolisib
mTOR, IC50: 1.6 nM
  99.68%
PF-04691502
mTOR, Ki: 16 nM
  99.91%
Paxalisib
mTOR, Ki: 70 nM
  99.63%
hSMG-1 inhibitor 11e
mTOR, IC50: 45 nM
  99.81%
Samotolisib
mTOR, IC50: 165 nM
  99.27%
Apitolisib
mTOR, Ki: 17 nM
  99.29%
Bimiralisib
mTOR, IC50: 89 nM
  99.80%
CC-115
mTOR, IC50: 21 nM
  99.82%
Dactolisib Tosylate
mTOR, IC50: 20.7 nM
  99.87%
Voxtalisib
mTOR, IC50: 157 nM
mTORC1, IC50: 160 nM
mTORC2, IC50: 910 nM
99.02%
Onatasertib
mTOR, IC50: 16 nM
  99.13%
BGT226
mTOR
  99.51%
GSK1059615
mTOR, IC50: 12 nM
  ≥99.0%
WYE-132
mTOR, IC50: 0.19 nM
  99.90%
Ridaforolimus 
mTOR
 99.75%
mTOR inhibitor-3
mTOR, Ki: 1.5 nM
  99.09%
PKI-402
mTOR, IC50: 3 nM
  98.43%
PP121
mTOR, IC50: 10 nM
  98.67%
OSI-027
mTOR, IC50: 4 nM
mTORC1, IC50: 22 nM
mTORC2, IC50: 65 nM
99.95%
VS-5584
mTOR, IC50: 37 nM
  99.14%
GNE-317
mTOR
  99.14%
PI-103 Hydrochloride 
mTORC1, IC50: 20 nM
mTORC2, IC50: 83 nM
98.55%
CZ415
mTOR, pIC50: 8.07
  98.39%
PQR530
mTOR, Kd: 0.33 nM
  99.98%
BGT226 maleate
mTOR
  99.92%
(+)-Usnic acid 
mTORC1
mTORC2
99.63%
ETP-46464
mTOR, IC50: 0.6 nM
  99.55%
Palomid 529 
TORC1
TORC2
99.37%
CC-115 hydrochloride
mTOR, IC50: 21 nM
  98.03%
PQR620 
mTORC1
mTORC2
98.01%
GDC-0349
mTOR, Ki: 3.8 nM
  98.02%
PF-04979064
mTOR, Ki: 1.42 nM
  99.54%
GNE-493
mTOR, IC50: 30 nM
  99.81%
WAY-600
mTOR, IC50: 9 nM
  99.75%
WYE-354
mTOR, IC50: 5 nM
  98.04%
HDACs/mTOR Inhibitor 1
mTOR, IC50: 1.2 nM
  99.01%
PI3K/mTOR Inhibitor-2
mTOR, IC50: 4.7 nM
  99.10%
Hederacolchiside A1
mTOR
  ≥99.0%
NSC781406
mTOR, IC50: 5.4 nM
  99.97%
MTI-31
mTOR, Ki: 0.2 nM
mTOR, IC50: 39 nM (100 μM ATP)
  99.98%
mTOR inhibitor-8
mTOR
  98.14%
MT 63-78 
mTORC1
 98.50%
PI3K/mTOR Inhibitor-4
mTOR, IC50: 13.85 nM
  
GNE-477
mTOR, Ki: 21 nM
  98.75%
ETP-45658
mTOR, IC50: 152.0 nM
  98.97%
PKI-179
mTOR, IC50: 0.42 nM
  ≥98.0%
Zederone
mTOR
  99.61%
Rotundic acid
mTOR
  99.41%
XL388
mTOR, IC50: 9.9 nM
  99.74%
FT-1518 
mTORC1
mTORC2
98.62%
HTH-01-091
mTOR, IC50: 632 nM
  98.64%
AZD3147 
mTORC1
mTORC2
99.93%
WYE-687
mTOR, IC50: 7 nM
  98.05%
TML-6
mTOR
  99.01%
PKI-179 hydrochloride
mTOR, IC50: 0.42 nM
  99.66%
CC214-2 
mTORC1
mTORC2
98.41%
8-Aminoadenosine
mTOR
  99.94%
GNE-490
mTOR, IC50: 750 nM
  
PI3K-IN-37
mTOR, IC50: 4 nM
  ≥99.0%
Pomiferin
mTOR, IC50: 6.2 μM
  98.98%
PI3K-IN-22
mTOR, IC50: 0.6 nM
  99.50%
WYE-687 dihydrochloride
mTOR, IC50: 7 nM
  ≥98.0%
Coronarin A 
mTORC1
 ≥98.0%
PI3K-IN-18
mTOR, IC50: 49 nM
  ≥99.0%
FD274
mTOR, IC50: 2.03 nM
  99.45%
PI3Kα/mTOR-IN-1
mTOR, Ki: 10.6 nM
  99.30%
HSP90/mTOR-IN-1
mTOR, IC50: 29 nM
  
PI3K/mTOR Inhibitor-1
mTOR, IC50: 186 nM
  
mTOR inhibitor-2
mTOR, IC50: 7 nM
  
PI3K/mTOR Inhibitor-9
mTOR, IC50: 38 nM (phospho-S6 cellular assay)
mTOR, IC50: 16 nM (Ser240/244 cellular assay)
  
SN32976
mTOR, IC50: 194 nM
  99.49%
ATM Inhibitor-3
mTOR
  
ATM Inhibitor-4
mTOR
  
mTOR/HDAC-IN-1
mTOR, IC50: 0.49 nM
  
PI3K/mTOR Inhibitor-3
mTOR
  
PI3Kα-IN-5
mTOR, IC50: 3.3 nM
  
PI3K/mTOR Inhibitor-12
mTOR, IC50: 3.12 nM
  
PI3K/mTOR Inhibitor-8
mTOR, IC50: 12 nM
  
ATR-IN-20
mTOR, IC50: 18 nM
  
Antifungal agent 106
mTOR, IC50: 0.8 μM
  
PI3K/mTOR Inhibitor-14
mTOR, IC50: 10.1 nM
  
mTOR/HDAC6-IN-1
mTOR, IC50: 133.7 nM
  
mTOR inhibitor-13
mTOR, IC50: 0.29 nM
  
mTOR inhibitor-17
mTOR, IC50: 0.68 nM
  
mTOR inhibitor-16
mTOR, IC50: 1.25 nM
  
mTOR inhibitor-10
mTOR, IC50: 0.7 nM