1. Signaling Pathways
  2. PI3K/Akt/mTOR
  3. 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-175646
    AGPAT4-IN-1
    Inhibitor
    AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. AGPAT4-IN-1 covalently binds to AGPAT4 at Cys228 and significantly inhibits acyltransferase activity, LPA-to-PA conversion and downstream mTOR/S6K pathways. AGPAT4-IN-1 sensitizes hepatocellular carcinoma (HCC) tumors to Sorafenib (HY-10201) and significantly induces apoptosis with a synergistic response. AGPAT4-IN-1 has antitumor activity and reduces tumorigenicity and stemness in HCC xenograft mouse models.
    AGPAT4-IN-1
  • HY-169022
    4-FPBUA
    Inhibitor
    4-FPBUA is a semisynthetic analog of usnic acid (HY-W015883) that can enhance cellular blood-brain barrier (BBB) function and increase the transport of Amyloid β (Aβ) across monolayer cells. 4-FPBUA is also an inhibitor of mTOR, capable of enhancing cellular Autophagy, thereby reversing BBB disruption in vivo and being utilized in research for Alzheimer's disease.
    4-FPBUA
  • HY-154910
    CC214-1
    Inhibitor 98.49%
    CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ,with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study.
    CC214-1
  • HY-121726
    3HOI-BA-01
    Inhibitor
    3HOI-BA-01 is amTORinhibitor.3HOI-BA-01reduces infarct size and inducedautophagyin a murine myocardial ischemia/reperfusion injury model.
    3HOI-BA-01
  • HY-N0656AR
    (+)-Usnic acid (Standard)
    Inhibitor
    (+)-Usnic acid (Standard) is the analytical standard of (+)-Usnic acid. This product is intended for research and analytical applications. (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium.
    (+)-Usnic acid (Standard)
  • HY-15901A
    LGB321 monohydrochloride
    Inhibitor
    LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies.
    LGB321 monohydrochloride
  • HY-108959
    D-87503
    Inhibitor
    D-87503 is a potent inhibitor of PI3k/Akt/mTOR, with the IC50s of 62 nM and 0.76 μM, respectively for PI3k and Erk2. D-87503 effectively suppressed the target downstream substrates Akt and Rsk1 kinase of the PI3k/Akt/mTOR signaling pathway.
    D-87503
  • HY-N12124
    Monascuspiloin
    Inhibitor
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice.
    Monascuspiloin
  • HY-N0486S13
    L-Leucine-15N,d10
    L-Leucine-15N,d10 is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
    L-Leucine-<sup>15</sup>N,d<sub>10</sub>
  • HY-139832
    MCX 28
    Inhibitor
    MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
    MCX 28
  • HY-W742805
    Sulindac Sulfone-d6
    Sulindac Sulfone-d6 is the deuterium labeled Sulindac sulfone (HY-B1787). 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-</sub>d<sub>6</sub>
  • HY-101776
    Desmethyl-VS-5584
    Inhibitor
    Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure.
    Desmethyl-VS-5584
  • HY-162993
    HN2210
    Inhibitor
    HN2210 is an mTORC2 inhibitor..
    HN2210
  • HY-N0486S5
    L-Leucine-2-13C
    Activator
    L-Leucine-2-13C is the 13C-labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.
    L-Leucine-2-<sup>13</sup>C
  • HY-15901
    LGB321
    Inhibitor
    LGB321 is an inhibitor of PIM2-dependent multiple myeloma cell lines, effectively inhibiting proliferation and key signaling pathways such as mTOR-C1 and phosphorylation of BAD.
    LGB321
  • HY-112774A
    ICSN3250 hydrochloride
    Inhibitor
    ICSN3250 hydrochloride is a halitulin analogue and a selective mTORC1 inhibitor. ICSN3250 hydrochloride directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 hydrochloride shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 hydrochloride specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 hydrochloride can be used for the study of cancer .
    ICSN3250 hydrochloride
  • HY-N0171AR
    Beta-Sitosterol (purity>98%) (Standard)
    Agonist
    Beta-Sitosterol (purity>98%) (Standard) is an analytical standard for Beta-Sitosterol (purity>98%). Beta-Sitosterol (purity>98%) is intended for research and analytical applications. Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
    Beta-Sitosterol (purity>98%) (Standard)
  • HY-176854
    PI3K/mTOR-IN-18
    Inhibitor
    PI3K/mTOR-IN-18 (Compound 12) is a highly selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-18 shows antitumor effects via competitive binding to PI3Kα (Ki=0.130 nM) and mTOR (Ki=0.111 nM). PI3K/mTOR-IN-18 blocks the PI3K/AKT/mTOR pathway and inhibits tumor cell proliferation (IC50=144 nM). PI3K/mTOR-IN-18 is promising for research of solid tumors (e.g., breast, NSCLC).
    PI3K/mTOR-IN-18
  • HY-156445
    PI3K/mTOR Inhibitor-14
    Inhibitor
    PI3K/mTOR Inhibitor-14 (compound Y-2) is a potent PI3K and mTOR dual inhibitor with IC50s of 171.4 nM and 10.1 nM, respectively. PI3K/mTOR Inhibitor-14 has antitumor activities.
    PI3K/mTOR Inhibitor-14
  • HY-144449
    mTOR/HDAC6-IN-1
    Inhibitor
    mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC).
    mTOR/HDAC6-IN-1
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.

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