Signaling Pathway

mTOR

mTOR

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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 insulin, 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 Inhibitors & Modulators (49)

Product Name Catalog No. Brief Description
AP1903

HY-16046

AP1903 is a homodimer binding to FKBP; elicites potent and dosedependent apoptotic death of engineered cell line HT1080 in culture with an EC50 of  0.1 nM
IC50 value: 0.1 nM (EC50, HT1080) [1]
Target: FKBP regulator
AP1903 is a ideal reagents for controlling the activities of cells that have been modified by gene therapy procedures, without interference from endogenous FKBP.

AP20187

HY-13992

AP20187 is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain.

AZD-8055

HY-10422

AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (~1,000-fold) against PI3K isoforms and ATM/DNA-PK.

AZD2014

HY-15247

AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms (α/β/γ/δ).

BEZ235

HY-50673

BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively; inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1.

BEZ235 Tosylate

HY-15174

BEZ235 tosylate(NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively; inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1.

CC-115

HY-16962

CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

CC-115 hydrochloride

HY-16962A

CC-115 hydrochloride is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

CC-223

HY-16956

CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3Kα (IC50=4 μM).

CZ415

HY-100222

CZ415 is a potent and highly selective mTOR inhibitor.

Deforolimus

HY-50908

Deforolimus(AP23573; MK-8669; Ridaforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin.

Dihydromyricetin

HY-N0112

Dihydromyricetin(Ampeloptin) is a flavonoid compound which possesses potent antitumor activity.

ETP-46464

HY-15521

ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively).

Everolimus

HY-10218

Everolimus (RAD001) is a mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

GDC-0084

HY-19962

GDC-0084 is a potent, selective inhibitor of Class I PI3K and mTOR with good penetration across the blood-brain barrier.

GDC-0349

HY-15248

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.

GDC-0980

HY-13246

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively; also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

GNE-317

HY-12763

GNE-317 is a potent  PI3K/mTOR inhibitor that can cross the blood–brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.

GNE-477

HY-11042

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.

GNE-493

HY-10811

GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively.