mTOR

Mammalian target of Rapamycin

mTOR

mTOR Isoform Specific Products:

mTOR Isoform Comparison

mTOR Related Products (418)
Antibodies (14)
mTOR Signaling Pathway
mTOR Isoform Comparison

By Effects:	Control (1) Inhibitors (334) Substrate (1) Agonists (9) Degrader (1) Antagonist (1) Activators (38) Modulators (6) p53 Inhibitor (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-U00326

PI3Kα/mTOR-IN-1	Inhibitor	99.30%
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

HY-15960

PWT-33597 free base	Inhibitor
PWT-33597 (VDC-597) free base is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 free base is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 free base has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

HY-115507

NMac1	Inhibitor
NMac1 is an orally active Nm23/NDPK activator. NMac1 directly binds to Nm23-H1 and activates the NDPK activity of recombinant Nm23-H1 with an EC₅₀ of 10.7 uM. NMac1 induces AMPK activation and inhibits mTOR and ERK, leading to mitochondrial OXPHOS dysregulation and suppressing mitochondrial ROS production, which in turn induces mitochondrial dysfunction in MDA-MB-231 cells. NMac1 inhibits Complex I activity and suppresses changes in morphology and actin cytoskeleton organization following Rac1 activation in MDA-MB-231 cells. NMac1 inhibits tumor invasion, migration and metastasis. NMac1 is useful for studying metastatic tumors, such as breast cancer. NMac1 can be isolated from the ginger cassumunar Roxb.

HY-151137

HSP90/mTOR-IN-1	Inhibitor
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC₅₀ values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer.

HY-139142A

Simufilam dihydrochloride	Inhibitor
Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores NMDAR signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease.

HY-112602

PI3K/mTOR Inhibitor-1	Inhibitor
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC₅₀s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.

HY-B0725A

Doxepin
Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system. Doxepin has also been proposed as a protective factor against oxidative stress.

HY-B1232A

Metyrapone Tartrate	Modulator
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression.

HY-15960A

PWT-33597	Inhibitor
PWT-33597 (VDC-597) is a dual inhibitor of PI3Kα and mTOR, which can effectively block the signaling downstream of PI3K and mTOR. PWT-33597 is capable of inducing tumor cell apoptosis and inhibiting tumor growth. PWT-33597 has anti-tumor activity and can be used in the research of tumors such as renal cell carcinoma.

HY-111370

mTOR inhibitor-2	Inhibitor
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC₅₀ of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.

HY-N0486S11

L-Leucine-d	Activator
L-Leucine-d is the deuterium labeled L-Leucine. L-Leucine is an essential branched-chain amino acid (BCAA), which activates the mTOR signaling pathway.

HY-159517

PI3K/Akt/mTOR-IN-5	Inhibitor
PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis.

HY-169100

Antiproliferative agent-57
Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC₅₀=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues.

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.

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.

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.

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.

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.

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.

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.

SLC7A5 SLC3A2 Sestrin1/2 CASTOR1 CASTOR1 GATOR2 GATOR1 FLCN-FNIP2 RagA/B RagC/D mTORC1 p14 MP1 p18 v-ATPase SLC38A9 Glucose GLUT4 DNA Damage p53 Sestrin1/2 AMPK IKKβ LKB1 RHEB FKBP12 Rapamycin mTOR mTORC1 DEPTOR RAPTOR PRAS40 mLST8 TNF Receptor TNF Growth factors GFRs: EGFRs, IGF1R, Insulin Receptor, FGFR and Met SOS SHC GRB2 IRS1 PI3K Ras Raf MEK ERK RSK TSC2 TSC1 TBC1D7 REDD1 4EBP eIF4E S6K eIF4B PDCD4 SKAR ATF4 MTHFD2 CAD HIF1α Lipin1 ULK1 UVRAG/
ATG14L TFEB ERK5 PGC1-α Autophage Proteasome
assembly SREBP Glucose
metabolism Apoptosis FOXO1,3 GRB10 S6K PTEN PDK1 Akt SGK Ion
transport Rho kinase PKC Actin/
cytoskeleton TSC2 TSC1 TBC1D7 mTOR DEPTOR RICTOR mSIN1 PROTOR mLST8 RAC1 GSK-3β Wnt mTORC2

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.

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mTOR

mTOR

mTOR Isoform Specific Products:

mTOR Isoform Specific Products:

mTOR Related Products (418)

Antibodies (14)

mTOR Signaling Pathway

mTOR Isoform Comparison

mTOR Related Products (418):