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:
    607.62
  • Formula:
    C35H28F3N5O2
  • Solubility:
    Soluble to 1 mM in DMSO with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    1222998-36-8
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
  5. Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles.
    Galluzzi et al.
    Nat.Rev.Drug.Discov., 2017;
Citations:

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

59 Citations: Showing 1 - 10
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  1. Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals
    Authors: Kimura Et al.
    Nature Communications 2016;7:13130
  2. mTORC1-mediated inhibition of polycystin-1 expression drives renal cyst formation in tuberous sclerosis complex.
    Authors: Pema Et al.
    Mol Biol Cell 2016;7:10786
  3. Trehalose, sucrose and raffinose are novel activators of autophagy in human keratinocytes through an mTOR-independent pathway.
    Authors: Chen Et al.
    PLoS One 2016;6:28423
  4. 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 2016;5
  5. mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells.
    Authors: Saric Et al.
    Autophagy 2016;27:321
  6. A Founder Mutation in VPS11 Causes an Autosomal Recessive Leukoencephalopathy Linked to Autophagic Defects.
    Authors: Zhang Et al.
    Cell Rep 2016;12:e1005848
  7. 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 2016;11:e0156239
  8. Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics.
    Authors: Speranza Et al.
    Nat Chem Biol 2015;9:62
  9. 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 2015;9:217
  10. The mTORC1/4E-BP pathway coordinates hemoglobin production with L-leucine availability.
    Authors: Chung Et al.
    Mol Cancer Res 2015;8:ra34
  11. Autophagy restricts HIV-1 infection by selectively degrading Tat in CD4+ T lymphocytes.
    Authors: Sagnier Et al.
    J Virol 2015;89:615
  12. Autophagy regulates hepatocyte identity and epithelial-to-mesenchymal and mesenchymal-to-epithelial transitions promoting Snail degradation.
    Authors: Grassi Et al.
    Cell Death Dis 2015;6:e1880
  13. Regulation of autophagy by coordinated action of mTORC1 and protein phosphatase 2A.
    Authors: Wong Et al.
    Nat Commun 2015;6:8048
  14. Autophagy activation and protection from mitochondrial dysfunction in human chondrocytes.
    Authors: Figueroa Et al.
    Autophagy 2015;67:966
  15. SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.
    Authors: Rebsamen Et al.
    Autophagy 2015;519:477
  16. Diacylglycerol kinase-ζ regulates mTORC1 and lipogenic metabolism in cancer cells through SREBP-1.
    Authors: Torres-Ayuso Et al.
    Oncogenesis 2015;4:e164
  17. 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 2015;35:956
  18. Amino Acid-Dependent mTORC1 Regulation by the Lysosomal Membrane Protein SLC38A9.
    Authors: Jung Et al.
    Mol Cell Biol 2015;35:2479
  19. 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 2015;35:1921
  20. Cholesterol-mediated activation of acid sphingomyelinase disrupts autophagy in the retinal pigment epithelium.
    Authors: Toops Et al.
    J Exp Med 2015;26:41640
  21. PDK1 orchestrates early NK cell development through induction of E4BP4 expression and maintenance of IL-15 responsiveness.
    Authors: Yang Et al.
    J Clin Invest 2015;212:253
  22. Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle.
    Authors: Saqcena Et al.
    Autophagy 2015;14:2285
  23. A mechanism for asymmetric cell division resulting in proliferative asynchronicity.
    Authors: Dey-Guha Et al.
    Autophagy 2015;13:223
  24. Coactivator SRC-2-dependent metabolic reprogramming mediates prostate cancer survival and metastasis.
    Authors: Dasgupta Et al.
    Sci Signal 2015;125:1174
  25. Phosphoproteomic Analysis of KSHV-Infected Cells Reveals Roles of ORF45-Activated RSK during Lytic Replication.
    Authors: Avey Et al.
    PLoS Pathog 2015;11:e1004993
  26. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.
    Authors: Thorne Et al.
    Mol Biol Cell 2015;11:58
  27. PARK2-mediated mitophagy is involved in regulation of HBEC senescence in COPD pathogenesis.
    Authors: Ito Et al.
    Nature 2015;11:547
  28. Pharmacological inhibition of lysosomes activates the MTORC1 signaling pathway in chondrocytes in an autophagy-independent manner.
    Authors: Newton Et al.
    Autophagy 2015;11:1594
  29. mTORC2 regulates cardiac response to stress by inhibiting MST1.
    Authors: Sciarretta Et al.
    Elife 2015;11:125
  30. TNFAIP3 promotes survival of CD4 T cells by restricting MTOR and promoting autophagy.
    Authors: Matsuzawa Et al.
    Sci Rep 2015;11:1052
  31. Hedgehog signaling activates a positive feedback mechanism involving insulin-like growth factors to induce osteoblast differentiation.
    Authors: Shi Et al.
    Front Behav Neurosci 2015;112:4678
  32. Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis.
    Authors: Li Et al.
    J Exp Med 2014;9:e104809
  33. Fertilization-induced autophagy in mouse embryos is independent of mTORC1.
    Authors: Yamamoto Et al.
    Biol Reprod 2014;91:7
  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 2014;7:63
  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.
    Diabetes 2014;63:3404
  36. Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.
    Authors: Liang Et al.
    J Exp Med 2014;211:2249
  37. Estradiol and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells.
    Authors: Li Et al.
    BMC Biochem 2014;211:15
  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 2014;15:4
  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 2014;10:e1004196
  40. Development of a novel method for quantification of autophagic protein degradation by AHA labeling.
    Authors: Zhang Et al.
    PLoS Genet 2014;10:901
  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.
    Autophagy 2014;10:431
  42. Autophagy fosters myofibroblast differentiation through MTORC2 activation and downstream upregulation of CTGF.
    Authors: Bernard Et al.
    Cell Cycle 2014;10:2193
  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 2014;10:1637
  44. p53-directed translational control can shape and expand the universe of p53 target genes.
    Authors: Zaccara Et al.
    Cell Death Differ 2014;
  45. Live imaging and single-cell analysis reveal differential dynamics of autophagy and apoptosis.
    Authors: Xu Et al.
    Autophagy 2013;9:1418
  46. 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 2013;64:4361
  47. Stimulation of autophagy improves endoplasmic reticulum stress-induced diabetes.
    Authors: Bachar-Wikstrom Et al.
    Diabetes 2013;62:1227
  48. 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 2013;54:1662
  49. Epigenetic regulation of autophagy by the methyltransferase G9a.
    Authors: Narvajas Et al.
    Mol Cell Biol 2013;33:3983
  50. Suppression of lysosome function induces autophagy via a feedback down-regulation of MTOR complex 1 (MTORC1) activity.
    Authors: Li Et al.
    J Biol Chem 2013;288:35769
  51. mTOR complex 2 phosphorylates IMP1 cotranslationally to promote IGF2 production and the proliferation of mouse embryonic fibroblasts.
    Authors: Dai Et al.
    Genes Dev 2013;27:301
  52. SYK regulates mTOR signaling in AML.
    Authors: Carnevale Et al.
    Leukemia 2013;27:2118
  53. mTOR regulates phagosome and entotic vacuole fission.
    Authors: Krajcovic Et al.
    Mol Biol Cell 2013;24:3736
  54. Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion.
    Authors: Zhou Et al.
    Cell Res 2013;23:508
  55. Interaction between FIP200 and ATG16L1 distinguishes ULK1 complex-dependent and -independent autophagy.
    Authors: Gammoh Et al.
    Nat Struct Mol Biol 2013;20:144
  56. Rag GTPases mediate amino acid-dependent recruitment of TFEB and MITF to lysosomes.
    Authors: Martina and Puertollano
    J Cell Biol 2013;200:475
  57. MTORC1 functions as a transcriptional regulator of autophagy by preventing nuclear transport of TFEB.
    Authors: Martina Et al.
    Autophagy 2012;8:903
  58. 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 2012;287:17530
  59. Keap1 degradation by autophagy for the maintenance of redox homeostasis.
    Authors: Taguchi Et al.
    J Exp Bot 2012;109:13561
Expand to show all 59 Citations

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