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Wortmannin

Catalog #: 1232
63 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1232/1
1232/5
Wortmannin | CAS No. 19545-26-7 | Inositol Lipid Inhibitors
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Description: Potent, irreversible inhibitor of PI 3-kinase. Also inhibitor of PLK1
Alternative 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

Purity: ≥98%

Product Details
Citations (63)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
428.44
Formula:
C23H24O8
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. A novel and essential role for FcgammaRIIa in cancer cell-induced platelet activation.
    Mitrugno A, Williams D, Kerrigan S, Moran N
    Blood, 2013;123(2):249-60.
  2. Nerve growth factor regulates endothelial cell survival and pathological retinal angiogenesis
    M Troullinak, VI Alexaki, I Mitroulis, A Witt, A Klotzsche-, KJ Chung, T Chavakis, M Economopou
    J. Cell. Mol. Med., 2019;0(0):.
  3. JNK inhibitor SP600125 enhances TGF-beta-induced apoptosis of RBE human cholangiocarcinoma cells in a Smad-dependent manner.
    Lin Y, Zhang B, Liang H, Lu Y, Ai X, Zhang B, Chen X
    Mol Med Rep, 2013;8(6):1623-9.
  4. The homozygous CX3CR1-M280 mutation impairs human monocyte survival
    AL Collar, M Swamydas, M O'Hayre, MS Sajib, KW Hoffman, SP Singh, A Mourad, MD Johnson, EM Ferre, JM Farber, JK Lim, CM Mikelis, JS Gutkind, MS Lionakis
    JCI Insight, 2018;3(3):.
  5. Direct regulation of the proglucagon gene by insulin, leptin, and cAMP in embryonic versus adult hypothalamic neurons.

    Mol. Endocrinol., 2102;26(8):1339-55.
  6. Phenylbutyrate induces cathelicidin expression via the vitamin D receptor: Linkage to inflammatory and growth factor cytokines pathways.
    Kulkarni N, Yi Z, Huehnken C, Agerberth B, Gudmundsson G
    Mol Immunol, 2015;63(2):530-9.
  7. Myeloid PTEN deficiency protects livers from ischemia reperfusion injury by facilitating M2 macrophage differentiation.
    Yue S, Rao J, Zhu J, Busuttil R, Kupiec-Weglinski J, Lu L, Wang X, Zhai Y
    J Immunol, 2014;192(11):5343-53.
  8. RhoG protein regulates platelet granule secretion and thrombus formation in mice.
    Goggs R, Harper M, Pope R, Savage J, Williams C, Mundell S, Heesom K, Bass M, Mellor H, Poole A
    J Biol Chem, 2013;288(47):34217-29.
  9. Phosphatidylinositol 3,4-bisphosphate regulates neurite initiation and dendrite morphogenesis via actin aggregation
    SX Zhang, LH Duan, SJ He, GF Zhuang, X Yu
    Cell Res, 2017;0(0):.
  10. Role of focal adhesion tyrosine kinases in GPVI-dependent platelet activation and reactive oxygen species formation.
    Carrim N, Walsh T, Consonni A, Torti M, Berndt M, Metharom P
    PLoS ONE, 2014;9(11):e113679.
  11. 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
  12. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase.
    Powis et al.
    Cancer Res., 1994;54:2419
  13. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase.
    Liu et al.
    Chem.Biol., 2005;12:99
  14. In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin.
    Schultz et al.
    Anticancer Res., 1995;15:1135
  15. Histamine 2/3 receptor agonists alleviate perioperative neurocognitive disorders by inhibiting microglia activation through the PI3K/AKT/FoxO1 pathway in aged rats
    YN Chen, HH Sha, YW Wang, Q Zhou, P Bhuiyan, NN Li, YN Qian, HQ Dong
    J Neuroinflammation, 2020;17(1):217.

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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

  1. Pancreatic Ins content regulation by the estrogen receptor ER alpha.
    Authors: Alonso-Magdalena Et al.
    PLoS One  ;3:e2069
  2. 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
  3. The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner.
    Authors: Heberle Et al.
    Life Sci Alliance  2019;2
  4. 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
  5. Integrin CD11b negatively regulates Mincle-induced signaling via the Lyn-SIRPα-SHP1 complex.
    Authors: Zhang Et al.
    Exp Mol Med  2018;50:e439
  6. The homozygous CX3CR1-M280 mutation impairs human monocyte survival.
    Authors: Collar Et al.
    JCI Insight  2018;3
  7. Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus.
    Authors: Medrihan Et al.
    Neuron  2017;95:564
  8. 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
  9. 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
  10. Phosphatidylinositol-4,5-bisphosphate is required for KCNQ1/KCNE1 channel function but not anterograde trafficking.
    Authors: Royal Et al.
    PLoS One  2017;12:e0186293
  11. 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
  12. Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution.
    Authors: Lee Et al.
    Oncotarget  2016;7:11322
  13. 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
  14. SPECC1L deficiency results in increased adherens junction stability and reduced cranial neural crest cell delamination.
    Authors: Wilson Et al.
    Sci Rep  2016;6:17735
  15. Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models.
    Authors: Ahmed
    Physiological Reports  2016;4:e13069
  16. Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
    Authors: Li Et al.
    J Clin Invest  2016;126:389
  17. The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
    Authors: Sahay Et al.
    PLoS One  2015;6:20604
  18. Endothelial Rac1 is essential for hematogenous metastasis to the lung.
    Authors: Yao Et al.
    Sci Rep  2015;6:17501
  19. 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
  20. 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
  21. Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons.
    Authors: Ledonne Et al.
    Mol Psychiatry  2015;20:959
  22. Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor.
    Authors: Koutsioumpa Et al.
    Oncotarget  2015;14:19
  23. 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
  24. Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1.
    Authors: Jiang and Zsombok
    Front Neurosci  2014;7:270
  25. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase.
    Authors: Ruisanchez Et al.
    FASEB J  2014;28:880
  26. 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
  27. 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
  28. A novel and essential role for FcγRIIa in cancer cell-induced platelet activation.
    Authors: Mitrugno Et al.
    Blood  2014;123:249
  29. Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2.
    Authors: McAlpine Et al.
    Autophagy  2013;9:361
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. Cellular Ins resistance disrupts leptin-mediated control of neuronal signaling and transcription.
    Authors: Nazarians-Armavil Et al.
    Mol Endocrinol  2013;27:990
  36. 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
  37. The expression and relaxant effect of bitter taste receptors in human bronchi.
    Authors: Grassin-Delyle Et al.
    Respir Res  2013;14:134
  38. 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
  39. 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
  40. Endogenous urotensin II selectively modulates erectile function through eNOS.
    Authors: Bianca Et al.
    PLoS One  2012;7:e31019
  41. 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
  42. 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
  43. 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
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. 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
  50. Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus.
    Authors: Coba Et al.
    J Biol Chem  2008;283:34101
  51. 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
  52. The novel adipocytokine visfatin exerts direct cardioprotective effects.
    Authors: Lim Et al.
    J Cell Mol Med  2008;12:1395
  53. 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
  54. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol  2007;194:77
  55. Protein kinase C dependent inhibition of the heteromeric Kir4.1-Kir5.1 channel.
    Authors: Rojas Et al.
    Biochim Biophys Acta  2007;1768:2030
  56. 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
  57. 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
  58. 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
  59. Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
    Authors: O'Riordan Et al.
    J Neurosci  2006;26:4870
  60. Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus.
    Authors: Qiu Et al.
    Mol Cancer Ther  2006;26:12943
  61. 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
  62. 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
  63. 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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