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

mTOR

Mammalian target of Rapamycin

mTOR

Related Products

PDF 2.11 MB

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.

mTOR Isoform Specific Products:

mTOR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N1255A
    Scoulerine hydrochloride
    		Inhibitor
    Scoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer.
    Scoulerine hydrochloride
  • HY-147285
    PI3K/mTOR Inhibitor-9
    		Inhibitor
    PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively.
    PI3K/mTOR Inhibitor-9
  • HY-181059
    AMPK/mTOR modulator-1
    		Inhibitor
    AMPK/mTOR modulator-1, Ginsenoside derivative, is an orally active mTOR inhibitor and AMPK activator. AMPK/mTOR modulator-1 activates AMPK signaling with a Kd of 4.759 μM. AMPK/mTOR modulator-1 promotes M1-like tumor-associated macrophage polarization while suppressing M2-like polarization. AMPK/mTOR modulator-1 can enhance glycolysis. AMPK/mTOR modulator-1 significantly inhibits tumor progression and shows anti-inflammation activity. AMPK/mTOR modulator-1 can be used for the research of colorectal cancer.
    AMPK/mTOR modulator-1
  • HY-18953
    mTOR inhibitor-23
    		Inhibitor
    mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines.
    mTOR inhibitor-23
  • HY-168884
    AV457
    		Inhibitor
    AV457 is a potent and selective mTOR inhibitor with an IC50 value of 0.54 µM. AV457 inhibits cyst growth in polycystic kidney disease (PKD) organoids. AV457 decreases the protein expression of P-s6, P-p70s6 and don’t decreases the protein expression of P-AKT.
    AV457
  • HY-181650
    T133
    		Inhibitor
    T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer.
    T133
  • HY-174141
    LP-65
    		Inhibitor
    LP-65 is a dual inhibitor of MEK (IC50=83.2 nM) and mTOR (IC50=40.5 nM). LP-65 blocks MEK and mTOR signaling pathways and inhibits tumor cell proliferation and migration. LP-65 is promising for research of cancers.
    LP-65
  • HY-16397AS
    Phenformin-d5 hydrochloride
    		Inhibitor
    Phenformin-d5 (Phenethylbiguanide-d5) hydrochloride is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an orally active biguanide hypoglycemic agent. Phenformin hydrochloride inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin hydrochloride inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.
    Phenformin-d<sub>5</sub> hydrochloride
  • HY-127067
    Yuanhuadin
    		Inhibitor
    Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion.
    Yuanhuadin
  • HY-154958
    mTOR inhibitor-12
    		Inhibitor
    mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases.
    mTOR inhibitor-12
  • HY-180056
    CAII-IN-12
    		Inhibitor
    CAII-IN-12 (compound 6c) is a potent and selective carbonic anhydrase (CA) II and VII inhibitor (hCA II Ki = 47.8 nM, hCA VII Ki = 3.6 nM) with anti-epilepitic activity. CAII-IN-12 displays selectivity over hCA I (Ki = 370 nM). CAII-IN-12 exhibits potent anticonvulsant activity in both Pentylenetetrazol- and Pilocarpine (HY-B0726A)-induced seizure mouse models. CAII-IN-12 increases expression of KCC2 in the hippocampus, maintains neuronal integrity, and reduces mTOR activity. CAII-IN-12 can be used for epilepsy research.
    CAII-IN-12
  • HY-178431
    MT-44
    		Inhibitor
    MT-44 is a highly selective and potent mTOR inhibitor with an IC50 of 49.4 nM. MT-44 can inhibit cancer cells proliferation, migration and invasion. MT-44 can induce cells apoptosis and ROS production and cause G2/M phase arrest. MT-44 can activate the cGAS/STING pathway. MT-44 can be used for the research of cancer, such as triple-negative breast cancer.
    MT-44
  • HY-146016
    PI3K/mTOR Inhibitor-5
    		Inhibitor
    PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC50 values of 86.9 nM and 14.6 nM, respectively.
    PI3K/mTOR Inhibitor-5
  • HY-P990248
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
    		Inhibitor
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.
    Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1)
  • HY-P10833
    C-VGB3
    		Inhibitor
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.
    C-VGB3
  • HY-181097
    EGFR-IN-192
    		Inhibitor
    EGFR-IN-192 is an anticancer agent. EGFR-IN-192 inhibits EGFR (IC50: 0.12 μM), downregulates the HIF-VEGF and PI3K/AKT/mTOR pathways, upregulates the tumor suppressor gene PTEN, and induces cell cycle arrest and apoptosis in tumor cells. EGFR-IN-192 exhibits antitumor activity and can be used in tumor research.
    EGFR-IN-192
  • HY-168129
    GSK3β/mTOR modulator 1
    		Inhibitor
    GSK3β/MTOR MODULATOR 1 (Derivative 2) is the GSK3β/mTOR signaling channel regulator. GSK3β/MTOR MODULATOR 1 can be used for acute lung damage (ALI) and inflammation research.
    GSK3β/mTOR modulator 1
  • HY-108338
    PF-05139962
    		Inhibitor
    PF-05139962 is a cyclic sulfone mTOR kinase inhibitor. PF-05139962 exhibits potent mTOR (Ki = 5 nM, pS473 IC50 = 48 nM, pS6 IC50 = 6 nM) inhibitory activity and high selectivity.
    PF-05139962
  • HY-155721
    22-(4′-py)-JA
    		Inhibitor
    22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC).
    22-(4′-py)-JA
  • HY-144686
    ATM Inhibitor-3
    		Inhibitor
    ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability.
    ATM Inhibitor-3
Cat. No. Product Name / Synonyms Application Reactivity
All Rights Reserved.
Download mTOR Signaling Pathway Map.

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 Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.