Wortmannin (CAS 19545-26-7): R&D Systems
Catalog Number: 1232
Alternate Names: SL-2052
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
Biological Activity
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
  • M.Wt:
    428.44
  • Formula:
    C23H24O8
  • Solubility:
    Soluble to 50 mM in DMSO and to 5 mM in ethanol with gentle warming
  • Storage:
    Desiccate at -20°C
  • CAS No:
    19545-26-7
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.
Background References
  1. 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
  2. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.
    Powis et al.
    Cancer Res., 1994;54:2419
  3. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase.
    Liu et al.
    Chem.Biol., 2005;12:99
  4. In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin.
    Schultz et al.
    Anticancer Res., 1995;15:1135
Citations:

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

42 Citations: Showing 1 - 10
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  1. Pancreatic insulin content regulation by the estrogen receptor ER alpha.
    Authors: Alonso-Magdalena Et al.
    PLoS One ;3:e2069
  2. 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
  3. Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution.
    Authors: Lee Et al.
    Oncotarget 2016;7:11322
  4. 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
  5. SPECC1L deficiency results in increased adherens junction stability and reduced cranial neural crest cell delamination.
    Authors: Wilson Et al.
    Sci Rep 2016;6:17735
  6. Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.
    Authors: Ahmed
    Physiological Reports 2016;4:?e13069
  7. The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
    Authors: Sahay Et al.
    PLoS One 2015;6:20604
  8. Endothelial Rac1 is essential for hematogenous metastasis to the lung.
    Authors: Yao Et al.
    Sci Rep 2015;6:17501
  9. 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
  10. Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor.
    Authors: Koutsioumpa Et al.
    Oncotarget 2015;14:19
  11. 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
  12. Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1.
    Authors: Jiang and Zsombok
    Front Neurosci 2014;7:270
  13. 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
  14. 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
  15. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood 2014;123:249
  16. Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2.
    Authors: McAlpine Et al.
    Autophagy 2013;9:361
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res 2013;14:134
  23. 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
  24. 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
  25. Endogenous urotensin II selectively modulates erectile function through eNOS.
    Authors: Bianca Et al.
    PLoS One 2012;7:e31019
  26. 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
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol 2007;194:77
  36. 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
  37. 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
  38. 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
  39. Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
    Authors: O'Riordan Et al.
    J Neurosci 2006;26:4870
  40. Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus.
    Authors: Qiu Et al.
    Mol Cancer Ther 2006;26:12943
  41. 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
  42. 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
Expand to show all 42 Citations

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