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Boston Biochem/Torin 1/4247/10
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Boston Biochem
货号 / 
4247/10
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数    量:
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4000-520-616
Product Details
Citations (123)
Reviews (2)
Biological Activity Technical DataAdditional InformationBackground Product DatasheetsCalculators

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.Tocris products are intended for laboratory research use only, unless stated otherwise.

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. Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles.Galluzzi et al.Nat.Rev.Drug.Discov., 2017;
  3. The pharmacology of mTOR inhibition.Guertin and SabatiniSci.Signal., 2009;2:pe24
  4. 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
  5. mTOR complex 1 regulates lipin 1 localization to control the SREBP pathway.Peterson et al.Cell., 2011;146:408

Product Datasheets

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Citations for Torin 1

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

123Citations: Showing 1 - 10

  1. HIF1A and NFAT5 coordinate Na+-boosted antibacterial defense via enhanced autophagy and autolysosomal targeting.Authors: Neubert Et al.Autophagy2019;:1
  2. Lethal Poisoning of Cancer Cells by Respiratory Chain Inhibition plus Dimethyl α-Ketoglutarate.Authors: Sica Et al.Cell Rep2019;27:820
  3. Type 2 diabetes is associated with suppression of autophagy and lipid accumulation in β-cells.Authors: Ji Et al.J Cell Mol Med2019;23:2890
  4. Dysfunctional autophagy following exposure to pro-inflammatory cytokines contributes to pancreatic β-cell apoptosis.Authors: Lambelet Et al.Cell Death Dis2018;9:96
  5. Amino acids stimulate the endosome-to-Golgi trafficking through Ragulator and small GTPase Arl5.Authors: Shi Et al.Nat Commun2018;9:4987
  6. Is Ras a potential target in treatment against cutaneous squamous cell carcinoma?.Authors: Li Et al.J Cancer2018;9:3373
  7. mTOR-dependent phosphorylation controls TFEB nuclear export.Authors: Napolitano Et al.Nat Commun2018;9:3312
  8. Carbon monoxide-induced TFEB nuclear translocation enhances mitophagy/mitochondrial biogenesis in hepatocytes and ameliorates inflammatory liver injury.Authors: Kim Et al.Cell Death Dis2018;9:1060
  9. Phosphatidylinositol-5-Phosphate 4-Kinases Regulate Cellular Lipid Metabolism By Facilitating Autophagy.Authors: Lundquist Et al.Mol Cell2018;70:531
  10. PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells.Authors: Georgilis Et al.Cancer Cell2018;34:85
  11. Metabolic reprogramming of murine cardiomyocytes during autophagy requires the extracellular nutrient sensor decorin.Authors: Gubbiotti Et al.J Biol Chem2018;293:16940
  12. ULK1 O-GlcNAcylation Is Crucial for Activating VPS34 via ATG14L during Autophagy Initiation.Authors: Pyo Et al.Cell Rep2018;25:2878
  13. Autophagosomal YKT6 is required for fusion with lysosomes independently of syntaxin 17.Authors: Matsui Et al.J Cell Biol2018;217:2633
  14. Lysosomal Protein Lamtor1 Controls Innate Immune Responses via Nuclear Translocation of Transcription Factor EB.Authors: Hayama Et al.J Immunol2018;200:3790
  15. Integration of Distinct ShcA Signaling Complexes Promotes Breast Tumor Growth and Tyrosine Kinase Inhibitor Resistance.Authors: Ha Et al.Mol Cancer Res2018;16:894
  16. HEPES activates a MiT/TFE-dependent lysosomal-autophagic gene network in cultured cells: A call for caution.Authors: Tol Et al.Autophagy2018;14:437
  17. Role of the MAPK/cJun NH2-terminal kinase signaling pathway in starvation-induced autophagy.Authors: Barutcu Et al.Autophagy2018;14:1586
  18. Lifespan extension without fertility reduction following dietary addition of the autophagy activator Torin1 in Drosophila melanogaster.Authors: Mason Et al.PLoS One2018;13:e0190105
  19. Mapping the mammalian ribosome quality control complex interactome using proximity labeling approaches.Authors: Zuzow Et al.Mol Biol Cell2018;
  20. Tenovin-6 impairs autophagy by inhibiting autophagic flux.Authors: Yuan Et al.Cell Death Dis2017;8:e2608
  21. TBK1 Provides Context-Selective Support of the Activated AKT/mTOR Pathway in Lung Cancer.Authors: Cooper Et al.Cancer Res2017;77:5077
  22. Autophagosomal Content Profiling Reveals an LC3C-Dependent Piecemeal Mitophagy Pathway.Authors: Guerroue Et al.Mol Cell2017;68:786
  23. PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation.Authors: Gupta Et al.Mol Cell2017;65:999
  24. Akt regulation of glycolysis mediates bioenergetic stability in epithelial cells.Authors: Hung Et al.Elife2017;6
  25. DGAT1-Dependent Lipid Droplet Biogenesis Protects Mitochondrial Function during Starvation-Induced Autophagy.Authors: Nguyen Et al.Dev Cell2017;42:9
  26. PtdIns3P controls mTORC1 signaling through lysosomal positioning.Authors: Hong Et al.J Cell Biol2017;216:4217
  27. Tim-3 is a Marker of Plasmacytoid Dendritic Cell Dysfunction during HIV Infection and Is Associated with the Recruitment of IRF7 and p85 into Lysosomes and with the Submembrane Displacement of TLR9.Authors: Schwartz Et al.J Immunol2017;198:3181
  28. TORC1 and TORC2 converge to regulate the SAGA co-activator in response to nutrient availability.Authors: Laboucarié Et al.EMBO Rep2017;18:2197
  29. Deubiquitinase OTUD6B Isoforms Are Important Regulators of Growth and Proliferation.Authors: Sobol Et al.Mol Cancer Res2017;15:117
  30. The E3 ubiquitin ligase NEDD4 enhances killing of membrane-perturbing intracellular bacteria by promoting autophagy.Authors: Pei Et al.Autophagy2017;13:2041
  31. Loss of ULK1 increases RPS6KB1-NCOR1 repression of NR1H/LXR-mediated Scd1 transcription and augments lipotoxicity in hepatic cells.Authors: Sinha Et al.Autophagy2017;13:169
  32. The anti-tumor drug 2-hydroxyoleic acid (Minerval) stimulates signaling and retrograde transport.Authors: Torgersen Et al.Oncotarget2016;7:86871
  33. TSC loss distorts DNA replication programme and sensitises cells to genotoxic stress.Authors: Pai Et al.Oncotarget2016;7:85365
  34. Diagnostic and clinical relevance of the autophago-lysosomal network in human gliomas.Authors: Jennewein Et al.Oncotarget2016;7:20016
  35. Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signalsAuthors: Kimura Et al.Nature Communications2016;7:13130
  36. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly.Authors: Gandin Et al.Nat Commun2016;7:11127
  37. mTORC1-mediated inhibition of polycystin-1 expression drives renal cyst formation in tuberous sclerosis complex.Authors: Pema Et al.Mol Biol Cell2016;7:10786
  38. Trehalose, sucrose and raffinose are novel activators of autophagy in human keratinocytes through an mTOR-independent pathway.Authors: Chen Et al.PLoS One2016;6:28423
  39. LKB1 loss links serine metabolism to DNA methylation and tumorigenesis.Authors: Kottakis Et al.Nature2016;539:390
  40. 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 A2016;5
  41. Characterizing inactive ribosomes in translational profiling.Authors: LiuTranslation (Austin)2016;4:e1138018
  42. Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP.Authors: Ricoult Et al.Oncogene2016;35:1250
  43. TDP-43 loss of function increases TFEB activity and blocks autophagosome-lysosome fusion.Authors: Xia Et al.EMBO J2016;35:121
  44. A novel Rab10-EHBP1-EHD2 complex essential for the autophagic engulfment of lipid droplets.Authors: Li Et al.Sci Adv2016;2:e1601470
  45. Nutrient-regulated Phosphorylation of ATG13 Inhibits Starvation-induced Autophagy.Authors: Puente Et al.J Biol Chem2016;291:6026
  46. RACK1 Is an Interaction Partner of ATG5 and a Novel Regulator of Autophagy.Authors: Erbil Et al.J Biol Chem2016;291:16753
  47. mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells.Authors: Saric Et al.Autophagy2016;27:321
  48. nanoCAGE reveals 5' UTR features that define specific modes of translation of functionally related MTOR-sensitive mRNAs.Authors: Gandin Et al.Genome Res2016;26:636
  49. Involvement of PARK2-Mediated Mitophagy in Idiopathic Pulmonary Fibrosis Pathogenesis.Authors: Kobayashi Et al.J Immunol2016;197:504
  50. Neuronal gene repression in Niemann-Pick type C models is mediated by the c-Abl/HDAC2 signaling pathway.Authors: Contreras Et al.Biochim Biophys Acta2016;1859:269
  51. A Founder Mutation in VPS11 Causes an Autosomal Recessive Leukoencephalopathy Linked to Autophagic Defects.Authors: Zhang Et al.Cell Rep2016;12:e1005848
  52. Drosophila Mitf regulates the V-ATPase and the lysosomal-autophagic pathway.Authors: Bouche Et al.Autophagy2016;12:484
  53. Hypoxia promotes noncanonical autophagy in nucleus pulposus cells independent of MTOR and HIF1A signaling.Authors: Choi Et al.Autophagy2016;12:1631
  54. Iron overload causes endolysosomal deficits modulated by NAADP-regulated 2-pore channels and RAB7A.Authors: Fernández Et al.Autophagy2016;12:1487
  55. TFEB and TFE3 cooperate in the regulation of the innate immune response in activated macrophages.Authors: Pastore Et al.Autophagy2016;12:1240
  56. TP53INP2/DOR, a mediator of cell autophagy, promotes rDNA transcription via facilitating the assembly of the POLR1/RNA polymerase I preinitiation complex at rDNA promoters.Authors: Xu Et al.Autophagy2016;12:1118
  57. IL-15 activates mTOR and primes stress-activated gene expression leading to prolonged antitumor capacity of NK cells.Authors: Mao Et al.Blood2016;128:1475
  58. IBMPFD Disease-Causing Mutant VCP/p97 Proteins Are Targets of Autophagic-Lysosomal Degradation.Authors: Bayraktar Et al.PLoS One2016;11:e0164864
  59. 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 One2016;11:e0156239
  60. Trehalose upregulates progranulin expression in human and mouse models of GRN haploinsufficiency: a novel therapeutic lead to treat frontotemporal dementia.Authors: Holler Et al.Mol Neurodegener2016;11:46
  61. Activation of 5-HT7 receptor stimulates neurite elongation through mTOR, Cdc42 and actin filaments dynamics.Authors: Speranza Et al.Nat Chem Biol2015;9:62
  62. The MAPK and PI3K pathways mediate CNTF-induced neuronal survival and process outgrowth in hypothalamic organotypic cultures.Authors: Askvig and WattJ Cell Commun Signal2015;9:217
  63. The mTORC1/4E-BP pathway coordinates hemoglobin production with L-leucine availability.Authors: Chung Et al.Mol Cancer Res2015;8:ra34
  64. Autophagy restricts HIV-1 infection by selectively degrading Tat in CD4+ T lymphocytes.Authors: Sagnier Et al.J Virol2015;89:615
  65. Reinstating aberrant mTORC1 activity in Huntington's disease mice improves disease phenotypes.Authors: Lee Et al.Neuron2015;85:303
  66. Autophagy regulates hepatocyte identity and epithelial-to-mesenchymal and mesenchymal-to-epithelial transitions promoting Snail degradation.Authors: Grassi Et al.Cell Death Dis2015;6:e1880
  67. Regulation of autophagy by coordinated action of mTORC1 and protein phosphatase 2A.Authors: Wong Et al.Nat Commun2015;6:8048
  68. Autophagy activation and protection from mitochondrial dysfunction in human chondrocytes.Authors: Figueroa Et al.Autophagy2015;67:966
  69. SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1.Authors: Rebsamen Et al.Autophagy2015;519:477
  70. Diacylglycerol kinase-ζ regulates mTORC1 and lipogenic metabolism in cancer cells through SREBP-1.Authors: Torres-Ayuso Et al.Oncogenesis2015;4:e164
  71. Decorin is an autophagy-inducible proteoglycan and is required for proper in vivo autophagy.Authors: Gubbiotti Et al.Matrix Biol2015;48:14
  72. 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 Biol2015;35:956
  73. Amino Acid-Dependent mTORC1 Regulation by the Lysosomal Membrane Protein SLC38A9.Authors: Jung Et al.Mol Cell Biol2015;35:2479
  74. HIV-1 Tat alters neuronal autophagy by modulating autophagosome fusion to the lysosome: implications for HIV-associated neurocognitive disorders.Authors: Fields Et al.J Neurosci2015;35:1921
  75. La-related Protein 1 (LARP1) Represses Terminal Oligopyrimidine (TOP) mRNA Translation Downstream of mTOR Complex 1 (mTORC1).Authors: Fonseca Et al.J Biol Chem2015;290:15996
  76. Cholesterol-mediated activation of acid sphingomyelinase disrupts autophagy in the retinal pigment epithelium.Authors: Toops Et al.J Exp Med2015;26:41640
  77. Amyloid precursor protein (APP) affects global protein synthesis in dividing human cells.Authors: Sobol Et al.J Cell Physiol2015;230:1064
  78. PDK1 orchestrates early NK cell development through induction of E4BP4 expression and maintenance of IL-15 responsiveness.Authors: Yang Et al.J Clin Invest2015;212:253
  79. Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle.Authors: Saqcena Et al.Autophagy2015;14:2285
  80. A mechanism for asymmetric cell division resulting in proliferative asynchronicity.Authors: Dey-Guha Et al.Autophagy2015;13:223
  81. mTORC1-Induced HK1-Dependent Glycolysis Regulates NLRP3 Inflammasome Activation.Authors: Moon Et al.Cell Rep2015;12:102
  82. Coactivator SRC-2-dependent metabolic reprogramming mediates prostate cancer survival and metastasis.Authors: Dasgupta Et al.Sci Signal2015;125:1174
  83. Phosphoproteomic Analysis of KSHV-Infected Cells Reveals Roles of ORF45-Activated RSK during Lytic Replication.Authors: Avey Et al.PLoS Pathog2015;11:e1004993
  84. GSK-3 modulates cellular responses to a broad spectrum of kinase inhibitors.Authors: Thorne Et al.Mol Biol Cell2015;11:58
  85. PARK2-mediated mitophagy is involved in regulation of HBEC senescence in COPD pathogenesis.Authors: Ito Et al.Nature2015;11:547
  86. Pharmacological inhibition of lysosomes activates the MTORC1 signaling pathway in chondrocytes in an autophagy-independent manner.Authors: Newton Et al.Autophagy2015;11:1594
  87. mTORC2 regulates cardiac response to stress by inhibiting MST1.Authors: Sciarretta Et al.Elife2015;11:125
  88. TNFAIP3 promotes survival of CD4 T cells by restricting MTOR and promoting autophagy.Authors: Matsuzawa Et al.Sci Rep2015;11:1052
  89. Hedgehog signaling activates a positive feedback mechanism involving Ins-like growth factors to induce osteoblast differentiation.Authors: Shi Et al.Front Behav Neurosci2015;112:4678
  90. Tor Signaling Regulates Transcription of Amino Acid Permeases through a GATA Transcription Factor Gaf1 in Fission Yeast.Authors: Ma Et al.PLoS One2015;10:e0144677
  91. Rapamycin-insensitive up-regulation of adipocyte phospholipase A2 in tuberous sclerosis and lymphangioleiomyomatosis.Authors: Li Et al.J Exp Med2014;9:e104809
  92. Fertilization-induced autophagy in mouse embryos is independent of mTORC1.Authors: Yamamoto Et al.Biol Reprod2014;91:7
  93. The nutrient-responsive transcription factor TFE3 promotes autophagy, lysosomal biogenesis, and clearance of cellular debris.Authors: Martina Et al.Sci Signal2014;7:ra9
  94. 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 Mech2014;7:63
  95. 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.Diabetes2014;63:3404
  96. Regulation of YAP by mTOR and autophagy reveals a therapeutic target of tuberous sclerosis complex.Authors: Liang Et al.J Exp Med2014;211:2249
  97. OE and mTORC2 cooperate to enhance prostaglandin biosynthesis and tumorigenesis in TSC2-deficient LAM cells.Authors: Li Et al.BMC Biochem2014;211:15
  98. Mammalian target of Rapamycin inhibition and mycobacterial survival are uncoupled in murine macrophages.Authors: Zullo Et al.Proc Natl Acad Sci U S A2014;15:4
  99. 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 Pathog2014;10:e1004196
  100. Development of a novel method for quantification of autophagic protein degradation by AHA labeling.Authors: Zhang Et al.PLoS Genet2014;10:901
  101. 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.Autophagy2014;10:431
  102. Autophagy fosters myofibroblast differentiation through MTORC2 activation and downstream upregulation of CTGF.Authors: Bernard Et al.Cell Cycle2014;10:2193
  103. Japanese encephalitis virus replication is negatively regulated by autophagy and occurs on LC3-I- and EDEM1-containing membranes.Authors: Sharma Et al.Arthritis Rheumatol2014;10:1637
  104. p53-directed translational control can shape and expand the universe of p53 target genes.Authors: Zaccara Et al.Cell Death Differ2014;
  105. Live imaging and single-cell analysis reveal differential dynamics of autophagy and apoptosis.Authors: Xu Et al.Autophagy2013;9:1418
  106. ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.Authors: Montané and MenandNat Commun2013;64:4361
  107. Stimulation of autophagy improves endoplasmic reticulum stress-induced diabetes.Authors: Bachar-Wikstrom Et al.Diabetes2013;62:1227
  108. 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 Res2013;54:1662
  109. Selective targeting of human colon cancer stem-like cells by the mTOR inhibitor Torin-1.Authors: Francipane and LagasseOncotarget2013;4:1948
  110. Epigenetic regulation of autophagy by the methyltransferase G9a.Authors: Narvajas Et al.Mol Cell Biol2013;33:3983
  111. Inactivation of the mTORC1-eukaryotic translation initiation factor 4E pathway alters stress granule formation.Authors: Fournier Et al.Mol Cell Biol2013;33:2285
  112. Suppression of lysosome function induces autophagy via a feedback down-regulation of MTOR complex 1 (MTORC1) activity.Authors: Li Et al.J Biol Chem2013;288:35769
  113. mTOR complex 2 phosphorylates IMP1 cotranslationally to promote IGF2 production and the proliferation of mouse embryonic fibroblasts.Authors: Dai Et al.Genes Dev2013;27:301
  114. SYK regulates mTOR signaling in AML.Authors: Carnevale Et al.Leukemia2013;27:2118
  115. mTOR regulates phagosome and entotic vacuole fission.Authors: Krajcovic Et al.Mol Biol Cell2013;24:3736
  116. Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion.Authors: Zhou Et al.Cell Res2013;23:508
  117. Interaction between FIP200 and ATG16L1 distinguishes ULK1 complex-dependent and -independent autophagy.Authors: Gammoh Et al.Nat Struct Mol Biol2013;20:144
  118. Rag GTPases mediate amino acid-dependent recruitment of TFEB and MITF to lysosomes.Authors: Martina and PuertollanoJ Cell Biol2013;200:475
  119. mTORC1 controls mitochondrial activity and biogenesis through 4E-BP-dependent translational regulation.Authors: Morita Et al.Cell Metab2013;18:698
  120. WNT-LRP5 signaling induces Warburg effect through mTORC2 activation during osteoblast differentiation.Authors: Esen Et al.Cell Metab2013;17:745
  121. MTORC1 functions as a transcriptional regulator of autophagy by preventing nuclear transport of TFEB.Authors: Martina Et al.Autophagy2012;8:903
  122. 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 Chem2012;287:17530
  123. Keap1 degradation by autophagy for the maintenance of redox homeostasis.Authors: Taguchi Et al.J Exp Bot2012;109:13561

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Filter by:

We got expected effect on cells
By Anonymouson 04/03/2020
Application: Species:Mouse

0.076–500 nM Torin


inhibition of Torin in acute brain slices
By Anonymouson 01/10/2018
Application: Species:Mouse

We used Torin-1 to inhibit torin signalling, we got the expected effect on metabolic changes in acute brain slices


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2018-10-22
Athens Research & Technology自1986年以来一直在净化人类蛋白质和开发这些蛋白质 查看更多>
1. 焦磷酸二乙酯(DEPC):是一种强烈但不彻底的RNA酶抑制剂。它通过和RNA酶的活性基团组氨酸的咪唑环结合使蛋白质变性,从而抑制酶的活性。 2. 异硫氰酸胍:目前被认为是最有效的RNA酶抑制剂,它在裂解组织的同时也使RNA酶失活。它既可破坏细胞结构使核酸从核蛋白中解离出来,又对RNA酶有强烈的变性作用。 3. 氧钒核糖核苷复合物:由氧化钒离子和核苷形成的复合物,它和RNA酶结合形成过渡态类物质,几乎能完全抑制RNA酶的活性。 4.... 查看更多>
Caspase 激活的脱氧核糖核酸酶抑制剂(抗原)现货直销,快递发货,含票含运费,提供说明书,欢迎来电咨询. 查看更多>
血管紧张素转化酶抑制剂(ACEI)是一种抑制血管紧张素转化酶活性的化合物。血管紧张素转化酶催化血管紧张素I生成血管紧张素II,后者是强烈的血管收缩剂和肾上腺皮质类醛固酮释放的激活剂。... 查看更多>
EGFR(表皮生长因子受体)的小分子抑制剂已被广泛应用于肺癌治疗中。一小部分(3-13%)的非小细胞肺癌(NSCLC)已经被证明在ALK(间变性淋巴瘤激酶)基因中有重新排列。在过去的几年中,ALK抑制剂与传统的化疗相比,对ALK-阳性NSCLC的管理有显著益处。 查看更多>
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人血管活性肽酶抑制剂(VPI)ELISA试剂盒现货直销,快递发货,提供一对一的技术服务和免费代测服务 查看更多>
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广州柏赛柯生物技术有限公司在发布的Pepstatin(天冬氨酸蛋白酶抑制剂)26305-03-3供应信息,浏览与Pepstatin(天冬氨酸蛋白酶抑制剂)26305-03-3相关的产品或在搜索更多与Pepstatin(天冬氨酸蛋白酶抑制剂)26305-03-3相关的内容。 查看更多>
2017-08-29
水在自然界的分布很广,占地球表面是四分之三、江、河、湖、都被水覆盖,地层、大气及动物、植物也含有大量的水分。水是生物生存的基本条件之一。高吸水性材料,指可吸收数十倍至数百倍于自身质量的水的物质。... 查看更多>
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相关疾病:高血压慢性心力衰竭冠心病心肌梗死糖尿病1977年施贵宝公司科学家ondetti等根据血管紧张素转换酶底物的化学结构推测设计出ACE的活性部位模型,1981年全球第一个血管紧张素转换酶抑制剂类药物卡托普利上市并用于治疗高血压,被列入降压药物......

《血管紧张素转换酶抑制剂在心血管病中应用的中国专家共识》.PDF(242.69k)
以前生化方面的实验接触很少,最近做一个酶抑制剂筛选工作,酶活性通过生成物吸光度测定。查了一些文献,发现酶的用量和底物用量文献之间差别很大,我想问一下
1.对于抑制剂筛选工作(求ic50)是不是体系内酶与底物的量(底物应该是过量的)对实验结果影响不大。
2.如果要求算Km值,是不是需要知道反应产物的绝对量。反应时间文献上都是5分钟,反应速度就用反应产物量除以反应时间即可。
3.酶是进口分装的,规格5U,一次用不完,用PBS稀释后如何保存
谢谢
1、不可逆抑制剂:如烷化剂、有机磷、重金属盐、氰化物等
2、可逆抑制剂:包括
a、竞争性抑制剂,抑制剂与底物竞争性结合酶反应中心,使Km增大,而Vmax不变 b、非竞争性抑制剂,酶与抑制剂结合后还能与底物结合,但活性降低,使Vmax减小,而Km不变
c、反竞争性抑制剂,酶只能与底物结合后才能与抑制剂结合,Vmax与Km都减小
可逆抑制剂可用透析等方法除去,使酶恢复作用
(血管紧张素转换酶抑制剂)包括卡托普利,贝那普利,依那普利,培哚普利等;(血管紧张素Ⅱ受体拮抗剂)包括缬沙坦,氯沙坦,厄贝沙坦,坎地沙坦等。这两类药物除了降压的作用外还可保护肾功能消减尿蛋白,但是ACEI(血管紧张素转换酶抑制剂)主要的副作用是咳嗽和血管性水肿,此时可以换副作用相对较少的ARB(血管紧张素Ⅱ受体拮抗剂)。
这是本人给研究生讲课的有关酶抑制剂的幻灯,该幻灯图文并貌,有许多动画。本课程是以郭宗儒编蓍的《药物化学总论》为参考书。

下载地址:/pub/其他资料/药化ppt/
本人最近在做中药里酪氨酸酶抑制剂的筛选,存在一些疑惑,望大家帮忙解答。
1、测定酶比活力:底物需要过量么?测定时间多长?是否可以加入过量的底物,然后测定3min吸光度的增加值,从吸光度的变化值计算比活力。

2、在酶抑制剂筛选的过程中,是否需要保证底物过量?还是要水浴一定时间让反应完全?我看到文献说用终浓度为0.1μmol/mL的底物,终浓度为45U/ml的酶,我想问,假设总体积为1ml,那么终浓度为45U/ml的酶岂不是每分钟能转化4.8μmol的底物?那么0.1μmol/mL的底物不就几秒钟就反应完了?那么怎么测定初速度?
相关疾病:卵巢癌癌症研究人员报告,组蛋白去乙酰化酶抑制剂(HDACIs),包括丙戊酸和SAHA,有效地抑制了人类卵巢癌细胞的增生,并诱发了凋亡。&n......
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