Catalog Number: 4247
Chemical Name: 1-[4-[4-(1-Oxopropyl)-1-piperazinyl]-3-(trifluoromethyl)phenyl]-9-(3-quinolinyl)-benzo[h]-1,6-naphthyridin-2(1H)-one
Biological Activity
Potent and selective mTOR inhibitor (IC50 = 2 - 10 nM for mTORC1 and mTORC2). Displays 200-fold selectivity for mTOR over DNA-PK, ATM and hVps34. Induces autophagy in HeLa cells.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 1 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold under license from Whitehead Institute for Biomedical Research.
Background References
  1. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1.
    Thoreen CC, Kang SA, Chang JW et al.
    J Biol Chem
  2. The pharmacology of mTOR inhibition.
    Guertin and Sabatini
    Sci.Signal., 2009;2:pe24
  3. Discovery of 1-(4(-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
    Liu et al.
    J.Med.Chem., 2010;53:7146
  4. mTOR complex 1 regulates lipin 1 localization to control the SREBP pathway.
    Peterson et al.
    Cell., 2011;146:408

The citations listed below are publications that use Tocris products. Selected citations for Torin 1 include:

Showing Results 1 - 10 of 58

  1. mTORC1-mediated inhibition of polycystin-1 expression drives renal cyst formation in tuberous sclerosis complex.
    Authors: Pema Et al.
    Mol Biol Cell
  2. Trehalose, sucrose and raffinose are novel activators of autophagy in human keratinocytes through an mTOR-independent pathway.
    Authors: Chen Et al.
    PLoS One
  3. An evolutionarily conserved mechanism for cAMP elicited axonal regeneration involves direct activation of the dual leucine zipper kinase DLK.
    Authors: Hao Et al.
    Proc Natl Acad Sci U S A
  4. mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells.
    Authors: Saric Et al.
  5. A Founder Mutation in VPS11 Causes an Autosomal Recessive Leukoencephalopathy Linked to Autophagic Defects.
    Authors: Zhang Et al.
    Cell Rep
  6. The Loss of Lam2 and Npr2-Npr3 Diminishes the Vacuolar Localization of Gtr1-Gtr2 and Disinhibits TORC1 Activity in Fission Yeast.
    Authors: Ma Et al.
    PLoS One
  7. Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics.
    Authors: Speranza Et al.
    Nat Chem Biol
  8. The MAPK and PI3K pathways mediate CNTF-induced neuronal survival and process outgrowth in hypothalamic organotypic cultures.
    Authors: Askvig and Watt
    J Cell Commun Signal
  9. The mTORC1/4E-BP pathway coordinates hemoglobin production with L-leucine availability.
    Authors: Chung Et al.
    Mol Cancer Res
  10. Autophagy restricts HIV-1 infection by selectively degrading Tat in CD4+ T lymphocytes.
    Authors: Sagnier Et al.
    J Virol
  11. Autophagy regulates hepatocyte identity and epithelial-to-mesenchymal and mesenchymal-to-epithelial transitions promoting Snail degradation.
    Authors: Grassi Et al.
    Cell Death Dis
  12. Regulation of autophagy by coordinated action of mTORC1 and protein phosphatase 2A.
    Authors: Wong Et al.
    Nat Commun
  13. Autophagy activation and protection from mitochondrial dysfunction in human chondrocytes.
    Authors: Figueroa Et al.
  14. SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.
    Authors: Rebsamen Et al.
  15. Diacylglycerol kinase-ζ regulates mTORC1 and lipogenic metabolism in cancer cells through SREBP-1.
    Authors: Torres-Ayuso Et al.
  16. Regulation of the transcription factor EB-PGC1α axis by beclin-1 controls mitochondrial quality and cardiomyocyte death under stress.
    Authors: Ma Et al.
    Mol Cell Biol
  17. Amino Acid-Dependent mTORC1 Regulation by the Lysosomal Membrane Protein SLC38A9.
    Authors: Jung Et al.
    Mol Cell Biol
  18. HIV-1 Tat alters neuronal autophagy by modulating autophagosome fusion to the lysosome: implications for HIV-associated neurocognitive disorders.
    Authors: Fields Et al.
    J Neurosci
  19. Cholesterol-mediated activation of acid sphingomyelinase disrupts autophagy in the retinal pigment epithelium.
    Authors: Toops Et al.
    J Exp Med
  20. PDK1 orchestrates early NK cell development through induction of E4BP4 expression and maintenance of IL-15 responsiveness.
    Authors: Yang Et al.
    J Clin Invest
  21. Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle.
    Authors: Saqcena Et al.
  22. A mechanism for asymmetric cell division resulting in proliferative asynchronicity.
    Authors: Dey-Guha Et al.
  23. Coactivator SRC-2-dependent metabolic reprogramming mediates prostate cancer survival and metastasis.
    Authors: Dasgupta Et al.
    Sci Signal
  24. Phosphoproteomic Analysis of KSHV-Infected Cells Reveals Roles of ORF45-Activated RSK during Lytic Replication.
    Authors: Avey Et al.
    PLoS Pathog
  25. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    Mol Biol Cell
  26. PARK2-mediated mitophagy is involved in regulation of HBEC senescence in COPD pathogenesis.
    Authors: Ito Et al.
  27. Pharmacological inhibition of lysosomes activates the MTORC1 signaling pathway in chondrocytes in an autophagy-independent manner.
    Authors: Newton Et al.
  28. mTORC2 regulates cardiac response to stress by inhibiting MST1.
    Authors: Sciarretta Et al.
  29. TNFAIP3 promotes survival of CD4 T cells by restricting MTOR and promoting autophagy.
    Authors: Matsuzawa Et al.
    Sci Rep
  30. Hedgehog signaling activates a positive feedback mechanism involving insulin-like growth factors to induce osteoblast differentiation.
    Authors: Shi Et al.
    Front Behav Neurosci
  31. p53-directed translational control can shape and expand the universe of p53 target genes.
    Authors: Zaccara Et al.
    Cell Death Differ
  32. Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis.
    Authors: Li Et al.
    J Exp Med
  33. Fertilization-induced autophagy in mouse embryos is independent of mTORC1.
    Authors: Yamamoto Et al.
    Biol Reprod
  34. Oncogenic mutations in adenomatous polyposis coli (Apc) activate mechanistic target of rapamycin complex 1 (mTORC1) in mice and zebrafish.
    Authors: Valvezan Et al.
    Dis Model Mech
  35. Palmitate induces mRNA translation and increases ER protein load in islet β-cells via activation of the mammalian target of rapamycin pathway.
    Authors: Hatanaka Et al.
  36. Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.
    Authors: Liang Et al.
    J Exp Med
  37. Estradiol and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells.
    Authors: Li Et al.
    BMC Biochem
  38. Mammalian target of Rapamycin inhibition and mycobacterial survival are uncoupled in murine macrophages.
    Authors: Zullo Et al.
    Proc Natl Acad Sci U S A
  39. An invertebrate Warburg effect: a shrimp virus achieves successful replication by altering the host metabolome via the PI3K-Akt-mTOR pathway.
    Authors: Su Et al.
    PLoS Pathog
  40. Development of a novel method for quantification of autophagic protein degradation by AHA labeling.
    Authors: Zhang Et al.
    PLoS Genet
  41. Expression of the autophagy substrate SQSTM1/p62 is restored during prolonged starvation depending on transcriptional upregulation and autophagy-derived amino acids.
    Authors: Sahani Et al.
  42. Autophagy fosters myofibroblast differentiation through MTORC2 activation and downstream upregulation of CTGF.
    Authors: Bernard Et al.
    Cell Cycle
  43. Japanese encephalitis virus replication is negatively regulated by autophagy and occurs on LC3-I- and EDEM1-containing membranes.
    Authors: Sharma Et al.
    Arthritis Rheumatol
  44. Live imaging and single-cell analysis reveal differential dynamics of autophagy and apoptosis.
    Authors: Xu Et al.
  45. ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.
    Authors: Montané and Menand
    Nat Commun
  46. Stimulation of autophagy improves endoplasmic reticulum stress-induced diabetes.
    Authors: Bachar-Wikstrom Et al.
  47. Differential regulation of the expressions of the PGC-1α splice variants, lipins, and PPARα in heart compared to liver.
    Authors: Kok Et al.
    J Lipid Res
  48. Epigenetic regulation of autophagy by the methyltransferase G9a.
    Authors: Narvajas Et al.
    Mol Cell Biol
  49. Suppression of lysosome function induces autophagy via a feedback down-regulation of MTOR complex 1 (MTORC1) activity.
    Authors: Li Et al.
    J Biol Chem
  50. mTOR complex 2 phosphorylates IMP1 cotranslationally to promote IGF2 production and the proliferation of mouse embryonic fibroblasts.
    Authors: Dai Et al.
    Genes Dev
  51. SYK regulates mTOR signaling in AML.
    Authors: Carnevale Et al.
  52. mTOR regulates phagosome and entotic vacuole fission.
    Authors: Krajcovic Et al.
    Mol Biol Cell
  53. Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion.
    Authors: Zhou Et al.
    Cell Res
  54. Interaction between FIP200 and ATG16L1 distinguishes ULK1 complex-dependent and -independent autophagy.
    Authors: Gammoh Et al.
    Nat Struct Mol Biol
  55. Rag GTPases mediate amino acid-dependent recruitment of TFEB and MITF to lysosomes.
    Authors: Martina and Puertollano
    J Cell Biol
  56. MTORC1 functions as a transcriptional regulator of autophagy by preventing nuclear transport of TFEB.
    Authors: Martina Et al.
  57. Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling.
    Authors: Fonseca Et al.
    J Biol Chem
  58. Keap1 degradation by autophagy for the maintenance of redox homeostasis.
    Authors: Taguchi Et al.
    J Exp Bot
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