Torin 1

Cat. No. 4247

Torin 1 C35H28F3N5O2 [1222998-36-8]

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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.

Licensing Information

Sold under license from Whitehead Institute for Biomedical Research.

Technical Data

Soluble to 1 mM in DMSO with gentle warming
>98 %
Store at +4°C

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. . PMID: 28529316 .

Peterson et al (2011) mTOR complex 1 regulates lipin 1 localization to control the SREBP pathway. Cell. 146 408. PMID: 21816276.

Liu et al (2010) 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. J.Med.Chem. 53 7146. PMID: 20860370.

Guertin and Sabatini (2009) The pharmacology of mTOR inhibition. Sci.Signal. 2 pe24. PMID: 19383975.

Thoreen et al (2009) An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J.Biol.Chem. 284 8023. PMID: 19150980.

If you know of a relevant reference for Torin 1 please let us know.

Citations are publications that use Tocris products. Selected citations for Torin 1 include:

Chen et al (2016) Trehalose, sucrose and raffinose are novel activators of autophagy in human keratinocytes through an mTOR-independent pathway. PLoS One 6 28423. PMID: 27328819.

Hao et al (2016) An evolutionarily conserved mechanism for cAMP elicited axonal regeneration involves direct activation of the dual leucine zipper kinase DLK. Proc Natl Acad Sci U S A 5. PMID: 27268300.

Kimura et al (2016) Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals Nature Communications 7 13130. PMID: 27731330.

Ma et al (2016) The Loss of Lam2 and Npr2-Npr3 Diminishes the Vacuolar Localization of Gtr1-Gtr2 and Disinhibits TORC1 Activity in Fission Yeast. PLoS One 11 e0156239. PMID: 27227887.

Pema et al (2016) mTORC1-mediated inhibition of polycystin-1 expression drives renal cyst formation in tuberous sclerosis complex. Mol Biol Cell 7 10786. PMID: 26931735.

Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Autophagy 27 321. PMID: 26582390.

Zhang et al (2016) A Founder Mutation in VPS11 Causes an Autosomal Recessive Leukoencephalopathy Linked to Autophagic Defects. Cell Rep 12 e1005848. PMID: 27120463.

Askvig and Watt (2015) The MAPK and PI3K pathways mediate CNTF-induced neuronal survival and process outgrowth in hypothalamic organotypic cultures. J Cell Commun Signal 9 217. PMID: 25698661.

Avey et al (2015) Phosphoproteomic Analysis of KSHV-Infected Cells Reveals Roles of ORF45-Activated RSK during Lytic Replication. PLoS Pathog 11 e1004993. PMID: 26133373.

Chung et al (2015) The mTORC1/4E-BP pathway coordinates hemoglobin production with L-leucine availability. Mol Cancer Res 8 ra34. PMID: 25872869.

Dasgupta et al (2015) Coactivator SRC-2-dependent metabolic reprogramming mediates prostate cancer survival and metastasis. Sci Signal 125 1174. PMID: 25664849.

Dey-Guha et al (2015) A mechanism for asymmetric cell division resulting in proliferative asynchronicity. Autophagy 13 223. PMID: 25582703.

Fields et al (2015) HIV-1 Tat alters neuronal autophagy by modulating autophagosome fusion to the lysosome: implications for HIV-associated neurocognitive disorders. J Neurosci 35 1921. PMID: 25653352.

Figueroa et al (2015) Autophagy activation and protection from mitochondrial dysfunction in human chondrocytes. Autophagy 67 966. PMID: 25605458.

Grassi et al (2015) Autophagy regulates hepatocyte identity and epithelial-to-mesenchymal and mesenchymal-to-epithelial transitions promoting Snail degradation. Cell Death Dis 6 e1880. PMID: 26355343.

Ito et al (2015) PARK2-mediated mitophagy is involved in regulation of HBEC senescence in COPD pathogenesis. Nature 11 547. PMID: 25714760.

Jung et al (2015) Amino Acid-Dependent mTORC1 Regulation by the Lysosomal Membrane Protein SLC38A9. Mol Cell Biol 35 2479. PMID: 25963655.

Ma et al (2015) Regulation of the transcription factor EB-PGC1α axis by beclin-1 controls mitochondrial quality and cardiomyocyte death under stress. Mol Cell Biol 35 956. PMID: 25561470.

Matsuzawa et al (2015) TNFAIP3 promotes survival of CD4 T cells by restricting MTOR and promoting autophagy. Sci Rep 11 1052. PMID: 26043155.

Newton et al (2015) Pharmacological inhibition of lysosomes activates the MTORC1 signaling pathway in chondrocytes in an autophagy-independent manner. Autophagy 11 1594. PMID: 26259639.

Rebsamen et al (2015) SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1. Autophagy 519 477. PMID: 25561175.

Sagnier et al (2015) Autophagy restricts HIV-1 infection by selectively degrading Tat in CD4+ T lymphocytes. J Virol 89 615. PMID: 25339774.

Saqcena et al (2015) Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle. Autophagy 14 2285. PMID: 25945415.

Sciarretta et al (2015) mTORC2 regulates cardiac response to stress by inhibiting MST1. Elife 11 125. PMID: 25843706.

Shi et al (2015) Hedgehog signaling activates a positive feedback mechanism involving insulin-like growth factors to induce osteoblast differentiation. Front Behav Neurosci 112 4678. PMID: 25825734.

Speranza et al (2015) Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics. Nat Chem Biol 9 62. PMID: 25814944.

Thorne et al (2015) GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors. Mol Biol Cell 11 58. PMID: 25402767.

Toops et al (2015) Cholesterol-mediated activation of acid sphingomyelinase disrupts autophagy in the retinal pigment epithelium. J Exp Med 26 41640. PMID: 25378587.

Torres-Ayuso et al (2015) Diacylglycerol kinase-ζ regulates mTORC1 and lipogenic metabolism in cancer cells through SREBP-1. Oncogenesis 4 e164. PMID: 26302180.

Wong et al (2015) Regulation of autophagy by coordinated action of mTORC1 and protein phosphatase 2A. Nat Commun 6 8048. PMID: 26310906.

Yang et al (2015) PDK1 orchestrates early NK cell development through induction of E4BP4 expression and maintenance of IL-15 responsiveness. J Clin Invest 212 253. PMID: 25624444.

Bernard et al (2014) Autophagy fosters myofibroblast differentiation through MTORC2 activation and downstream upregulation of CTGF. Cell Cycle 10 2193. PMID: 25495560.

Hatanaka et al (2014) Palmitate induces mRNA translation and increases ER protein load in islet β-cells via activation of the mammalian target of rapamycin pathway. Diabetes 63 3404. PMID: 24834975.

Li et al (2014) Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis. J Exp Med 9 e104809. PMID: 25347447.

Li et al (2014) Estradiol and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells. BMC Biochem 211 15. PMID: 24395886.

Liang et al (2014) Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex. J Exp Med 211 2249. PMID: 25288394.

Sahani et al (2014) Expression of the autophagy substrate SQSTM1/p62 is restored during prolonged starvation depending on transcriptional upregulation and autophagy-derived amino acids. Autophagy 10 431. PMID: 24394643.

Sharma et al (2014) Japanese encephalitis virus replication is negatively regulated by autophagy and occurs on LC3-I- and EDEM1-containing membranes. Arthritis Rheumatol 10 1637. PMID: 25046112.

Su et al (2014) An invertebrate Warburg effect: a shrimp virus achieves successful replication by altering the host metabolome via the PI3K-Akt-mTOR pathway. PLoS Pathog 10 e1004196. PMID: 24945378.

Valvezan et al (2014) Oncogenic mutations in adenomatous polyposis coli (Apc) activate mechanistic target of rapamycin complex 1 (mTORC1) in mice and zebrafish. Dis Model Mech 7 63. PMID: 24092877.

Yamamoto et al (2014) Fertilization-induced autophagy in mouse embryos is independent of mTORC1. Biol Reprod 91 7. PMID: 24855105.

Zaccara et al (2014) p53-directed translational control can shape and expand the universe of p53 target genes. Cell Death Differ. PMID: 24926617.

Zhang et al (2014) Development of a novel method for quantification of autophagic protein degradation by AHA labeling. PLoS Genet 10 901. PMID: 24675368.

Zullo et al (2014) Mammalian target of Rapamycin inhibition and mycobacterial survival are uncoupled in murine macrophages. Proc Natl Acad Sci U S A 15 4. PMID: 24528777.

Bachar-Wikstrom et al (2013) Stimulation of autophagy improves endoplasmic reticulum stress-induced diabetes. Diabetes 62 1227. PMID: 23274896.

Carnevale et al (2013) SYK regulates mTOR signaling in AML. Leukemia 27 2118. PMID: 23535559.

Dai et al (2013) mTOR complex 2 phosphorylates IMP1 cotranslationally to promote IGF2 production and the proliferation of mouse embryonic fibroblasts. Genes Dev 27 301. PMID: 23388827.

Gammoh et al (2013) Interaction between FIP200 and ATG16L1 distinguishes ULK1 complex-dependent and -independent autophagy. Nat Struct Mol Biol 20 144. PMID: 23262492.

Kok et al (2013) Differential regulation of the expressions of the PGC-1α splice variants, lipins, and PPARα in heart compared to liver. J Lipid Res 54 1662. PMID: 23505321.

Krajcovic et al (2013) mTOR regulates phagosome and entotic vacuole fission. Mol Biol Cell 24 3736. PMID: 24088573.

Li et al (2013) Suppression of lysosome function induces autophagy via a feedback down-regulation of MTOR complex 1 (MTORC1) activity. J Biol Chem 288 35769. PMID: 24174532.

Martina and Puertollano (2013) Rag GTPases mediate amino acid-dependent recruitment of TFEB and MITF to lysosomes. J Cell Biol 200 475. PMID: 23401004.

Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. Nat Commun 64 4361. PMID: 23963679.

Narvajas et al (2013) Epigenetic regulation of autophagy by the methyltransferase G9a. Mol Cell Biol 33 3983. PMID: 23918802.

Xu et al (2013) Live imaging and single-cell analysis reveal differential dynamics of autophagy and apoptosis. Autophagy 9 1418. PMID: 23748697.

Zhou et al (2013) Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion. Cell Res 23 508. PMID: 23337583.

Fonseca et al (2012) Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling. J Biol Chem 287 17530. PMID: 22474287.

Martina et al (2012) MTORC1 functions as a transcriptional regulator of autophagy by preventing nuclear transport of TFEB. Autophagy 8 903. PMID: 22576015.

Taguchi et al (2012) Keap1 degradation by autophagy for the maintenance of redox homeostasis. J Exp Bot 109 13561. PMID: 22872865.

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