Wortmannin
Chemical Name: (1S,6bR,9aS,11R,11bR) 11-(Acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b-dimethyl-3H-furo[4,3,2-de]indeno[4,5,-h]-2-h]-2-benzopyran-3,6,9-trione
Purity: ≥98%
Biological Activity
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM). Also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).Technical Data
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.
Background References
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Wortmannin is a potent phophatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses.
Arcaro and Wymann
Biochem.J., 1993;296:297 -
Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.
Powis et al.
Cancer Res., 1994;54:2419 -
Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase.
Liu et al.
Chem.Biol., 2005;12:99 -
In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin.
Schultz et al.
Anticancer Res., 1995;15:1135
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Citations for Wortmannin
The citations listed below are publications that use Tocris products. Selected citations for Wortmannin include:
63 Citations: Showing 1 - 10
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Pancreatic Ins content regulation by the estrogen receptor ER alpha.
Authors: Alonso-Magdalena Et al.
PLoS One ;3:e2069
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Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner.
Authors: Wijerathne Et al.
Korean J Physiol Pharmacol 2019;23:381
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The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner.
Authors: Heberle Et al.
Life Sci Alliance 2019;2
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Age-associated cholesterol reduction triggers brain Ins. resistance by facilitating ligand-independent receptor activation and pathway desensitization.
Authors: Martín-Segura Et al.
Aging Cell 2019;18:e12932
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Integrin CD11b negatively regulates Mincle-induced signaling via the Lyn-SIRPα-SHP1 complex.
Authors: Zhang Et al.
Exp Mol Med 2018;50:e439
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The homozygous CX3CR1-M280 mutation impairs human monocyte survival.
Authors: Collar Et al.
JCI Insight 2018;3
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Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus.
Authors: Medrihan Et al.
Neuron 2017;95:564
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Induction of Bex genes by curcumin is associated with apoptosis and activation of p53 in N2a neuroblastoma cells.
Authors: Sidhar and Giri
Sci Rep 2017;7:41420
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Molecular mechanisms involved in the non-monotonic effect of bisphenol-a on Ca2+ entry in mouse pancreatic β-cells.
Authors: Villar-Pazos Et al.
Sci Rep 2017;7:11770
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Phosphatidylinositol-4,5-bisphosphate is required for KCNQ1/KCNE1 channel function but not anterograde trafficking.
Authors: Royal Et al.
PLoS One 2017;12:e0186293
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PACAP and VIP Inhibit the Invasiveness of Glioblastoma Cells Exposed to Hypoxia through the Regulation of HIFs and EGFR Expression.
Authors: Maugeri Et al.
Oncotarget 2016;7:139
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Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution.
Authors: Lee Et al.
Oncotarget 2016;7:11322
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The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
Authors: Olianas Et al.
European Journal of Pharmacology 2016;794:135
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SPECC1L deficiency results in increased adherens junction stability and reduced cranial neural crest cell delamination.
Authors: Wilson Et al.
Sci Rep 2016;6:17735
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Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.
Authors: Ahmed
Physiological Reports 2016;4:e13069
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Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
Authors: Li Et al.
J Clin Invest 2016;126:389
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The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
Authors: Sahay Et al.
PLoS One 2015;6:20604
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Endothelial Rac1 is essential for hematogenous metastasis to the lung.
Authors: Yao Et al.
Sci Rep 2015;6:17501
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Stimulation of EphB2 attenuates tau phosphorylation through PI3K/Akt-mediated inactivation of glycogen synthase kinase-3β.
Authors: Jiang Et al.
Mol Cancer 2015;5:11765
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α6-Containing GABAA Receptors Are the Principal Mediators of Inhibitory Synapse Strengthening by Ins in Cerebellar Granule Cells.
Authors: Accardi Et al.
J Neurosci 2015;35:9676
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Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.
Authors: Ledonne Et al.
Mol Psychiatry 2015;20:959
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Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor.
Authors: Koutsioumpa Et al.
Oncotarget 2015;14:19
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Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
Authors: Rogers and Gahring
Front Pharmacol 2015;10:e0143319
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Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1.
Authors: Jiang and Zsombok
Front Neurosci 2014;7:270
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Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase.
Authors: Ruisanchez Et al.
FASEB J 2014;28:880
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Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na.
Authors: Mäki-Jouppila Et al.
Nat Commun 2014;13:1054
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Mechanosensitive ATP release from hemichannels and Ca2+ influx through TRPC6 accelerate wound closure in keratinocytes.
Authors: Takada Et al.
J Cell Sci 2014;127:4159
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A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
Authors: Mitrugno Et al.
Blood 2014;123:249
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Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2.
Authors: McAlpine Et al.
Autophagy 2013;9:361
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Combination of LC3 shRNA plasmid transfection and genistein treatment inhibited autophagy and increased apoptosis in malignant neuroblastoma in cell culture and animal models.
Authors: Mohan Et al.
PLoS One 2013;8:e78958
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Herpes simplex virus 2 (HSV-2) prevents dendritic cell maturation, induces apoptosis, and triggers release of proinflammatory cytokines: potential links to HSV-HIV synergy.
Authors: Stefanidou Et al.
Mol Immunol 2013;87:1443
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EI24 regulates epithelial-to-mesenchymal transition and tumor progression by suppressing TRAF2-mediated NF-κB activity.
Authors: Choi Et al.
J Virol 2013;4:2383
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An essential role for inhibitor-2 regulation of protein phosphatase-1 in synaptic scaling.
Authors: Siddoway Et al.
J Pharmacol Exp Ther 2013;33:11206
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Melatonin acts through MT1/MT2 receptors to activate hypothalamic Akt and suppress hepatic gluconeogenesis in rats.
Authors: Faria Et al.
Am J Physiol Endocrinol Metab 2013;305:E230
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Cellular Ins resistance disrupts leptin-mediated control of neuronal signaling and transcription.
Authors: Nazarians-Armavil Et al.
Mol Endocrinol 2013;27:990
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HSV activates Akt to trigger calcium release and promote viral entry: novel candidate target for treatment and suppression.
Authors: Cheshenko Et al.
FASEB J 2013;27:2584
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The expression and relaxant effect of bitter taste receptors in human bronchi.
Authors: Grassin-Delyle Et al.
Respir Res 2013;14:134
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The class I PI3K/Akt pathway is critical for cancer cell survival in dogs and offers an opportunity for therapeutic intervention.
Authors: Chen Et al.
BMC Vet Res 2012;8:73
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Long-lasting LTP requires neither repeated trains for its induction nor protein synthesis for its development.
Authors: Villers Et al.
PLoS One 2012;7:e40823
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Endogenous urotensin II selectively modulates erectile function through eNOS.
Authors: Bianca Et al.
PLoS One 2012;7:e31019
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An essential role for modulation of hyperpolarization-activated current in the development of binaural temporal precision.
Authors: Khurana Et al.
J Neurosci 2012;32:2814
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TNF-α triggers rapid membrane insertion of Ca(2+) permeable AMPA receptors into adult motor neurons and enhances their susceptibility to slow excitotoxic injury.
Authors: Yin Et al.
J Cell Sci 2012;238:93
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CDK5 is essential for soluble amyloid β-induced degradation of GKAP and remodeling of the synaptic actin cytoskeleton.
Authors: Roselli Et al.
PLoS One 2011;6:e23097
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Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor.
Authors: Huang Et al.
J Neurosci 2010;30:6080
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FRP inhibits ox-LDL-induced endothelial cell apoptosis through an Akt-NF-{kappa}B-Bcl-2 pathway and inhibits endothelial cell apoptosis in an apoE-knockout mouse model.
Authors: Liu Et al.
Am J Physiol Endocrinol Metab 2010;299:E351
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Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways.
Authors: Roselli Et al.
PLoS One 2009;4:e6011
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FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation.
Authors: Grodzki Et al.
Exp Neurol 2009;46:2539
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Inhibitory effect of ETB receptor on Na(+)-K(+) ATPase activity by extracellular Ca(2+) entry and Ca(2+) release from the endoplasmic reticulum in renal proximal tubule cells.
Authors: Liu Et al.
Hypertens Res 2009;32:846
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c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells.
Authors: Garcia Et al.
J Immunol 2009;183:4475
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Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus.
Authors: Coba Et al.
J Biol Chem 2008;283:34101
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Antigenic experience dictates functional role of glycogen synthase kinase-3 in human CD4+ T cell responses.
Authors: Garcia Et al.
J Immunol 2008;181:8363
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The novel adipocytokine visfatin exerts direct cardioprotective effects.
Authors: Lim Et al.
J Cell Mol Med 2008;12:1395
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Temporal profiling of changes in phosphatidylinositol 4,5-bisphosphate, inositol 1,4,5-trisphosphate and diacylglycerol allows comprehensive analysis of phospholipase C-initiated signalling in single neurons.
Authors: Nelson Et al.
J Neurochem 2008;107:602
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IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
Authors: Chung Et al.
J Endocrinol 2007;194:77
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Protein kinase C dependent inhibition of the heteromeric Kir4.1-Kir5.1 channel.
Authors: Rojas Et al.
Biochim Biophys Acta 2007;1768:2030
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PI-3-kinase-dependent membrane recruitment of centaurin-α2 is essential for its effect on ARF6-mediated actin cytoskeleton reorganisation.
Authors: Venkateswarlu Et al.
J Neurosci 2007;120:792
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GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis.
Authors: Lin Et al.
J Cell Sci 2007;120:2935
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Sphingosine 1-phosphate induces endothelial nitric-oxide synthase activation through phosphorylation in human corpus cavernosum.
Authors: Bianca Et al.
J Cell Biochem 2006;316:703
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Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
Authors: O'Riordan Et al.
J Neurosci 2006;26:4870
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Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus.
Authors: Qiu Et al.
Mol Cancer Ther 2006;26:12943
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Myosin light chain kinase is not a regulator of synaptic vesicle trafficking during repetitive exocytosis in cultured hippocampal neurons.
Authors: Tokuoka and Goda
J Neurosci 2006;26:11606
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LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II.
Authors: Searl and Silinsky
Purinergic Signal 2005;1:389
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Mechanisms underlying the relaxation response induced by bradykinin in the epithelium-intact guinea-pig trachea in vitro.
Authors: Schlemper Et al.
Br J Pharmacol 2005;145:740
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