Wortmannin

Cat. No. 1232

Wortmannin C23H24O8 [19545-26-7]

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Alternative Name: 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
Select another batch:

References are publications that support the products' biological activity.

Liu et al (2005) Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalian polo-like kinase. Chem.Biol. 12 99. PMID: 15664519.

Schultz et al (1995) In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin. Anticancer Res. 15 1135. PMID: 7653991.

Powis et al (1994) Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res. 54 2419. PMID: 8162590.

Arcaro and Wymann (1993) Wortmannin is a potent phophatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses. Biochem.J. 296 297. PMID: 8257416.

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

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

Lee et al (2016) Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution. Oncotarget 7 11322. PMID: 27089465.

Maugeri et al (2016) PACAP and VIP Inhibit the Invasiveness of Glioblastoma Cells Exposed to Hypoxia through the Regulation of HIFs and EGFR Expression. Oncotarget 7 139. PMID: 27303300.

Olianas et al (2016) The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors European Journal of Pharmacology 794 135. PMID: 27876620.

Wilson et al (2016) SPECC1L deficiency results in increased adherens junction stability and reduced cranial neural crest cell delamination. Sci Rep 6 17735. PMID: 26787558.

Jiang et al (2015) Stimulation of EphB2 attenuates tau phosphorylation through PI3K/Akt-mediated inactivation of glycogen synthase kinase-3β. Mol Cancer 5 11765. PMID: 26119563.

Koutsioumpa et al (2015) Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor. Oncotarget 14 19. PMID: 25644401.

Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. Front Pharmacol 10 e0143319. PMID: 26619345.

Sahay et al (2015) The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer. PLoS One 6 20604. PMID: 26098771.

Yao et al (2015) Endothelial Rac1 is essential for hematogenous metastasis to the lung. Sci Rep 6 17501. PMID: 25991673.

Jiang and Zsombok (2014) Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1. Front Neurosci 7 270. PMID: 24454277.

Mäki-Jouppila et al (2014) Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na. Nat Commun 13 1054. PMID: 24748653.

Mitrugno et al (2014) A novel and essential role for FcγRIIa in cancer cell-induced platelet activation. Blood 123 249. PMID: 24258815.

Takada et al (2014) Mechanosensitive ATP release from hemichannels and Ca2+ influx through TRPC6 accelerate wound closure in keratinocytes. J Cell Sci 127 4159. PMID: 25097230.

Cheshenko et al (2013) HSV activates Akt to trigger calcium release and promote viral entry: novel candidate target for treatment and suppression. FASEB J 27 2584. PMID: 23507869.

Choi et al (2013) EI24 regulates epithelial-to-mesenchymal transition and tumor progression by suppressing TRAF2-mediated NF-κB activity. J Virol 4 2383. PMID: 24280371.

Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134. PMID: 24266887.

McAlpine et al (2013) Regulation of nutrient-sensitive autophagy by uncoordinated 51-like kinases 1 and 2. Autophagy 9 361. PMID: 23291478.

Mohan et al (2013) Combination of LC3 shRNA plasmid transfection and genistein treatment inhibited autophagy and increased apoptosis in malignant neuroblastoma in cell culture and animal models. PLoS One 8 e78958. PMID: 24205354.

Siddoway et al (2013) An essential role for inhibitor-2 regulation of protein phosphatase-1 in synaptic scaling. J Pharmacol Exp Ther 33 11206. PMID: 23825423.

Stefanidou et al (2013) Herpes simplex virus 2 (HSV-2) prevents dendritic cell maturation, induces apoptosis, and triggers release of proinflammatory cytokines: potential links to HSV-HIV synergy. Mol Immunol 87 1443. PMID: 23152529.

Bianca et al (2012) Endogenous urotensin II selectively modulates erectile function through eNOS. PLoS One 7 e31019. PMID: 22319601.

Chen et al (2012) The class I PI3K/Akt pathway is critical for cancer cell survival in dogs and offers an opportunity for therapeutic intervention. BMC Vet Res 8 73. PMID: 22647622.

Khurana et al (2012) An essential role for modulation of hyperpolarization-activated current in the development of binaural temporal precision. J Neurosci 32 2814. PMID: 22357864.

Villers et al (2012) Long-lasting LTP requires neither repeated trains for its induction nor protein synthesis for its development. PLoS One 7 e40823. PMID: 22792408.

Yin et al (2012) TNF-α triggers rapid membrane insertion of Ca(2+) permeable AMPA receptors into adult motor neurons and enhances their susceptibility to slow excitotoxic injury. J Cell Sci 238 93. PMID: 22921461.

Liu et al (2010) 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. Am J Physiol Endocrinol Metab 299 E351. PMID: 20530739.

Garcia et al (2009) c-jun controls the ability of IL-12 to induce IL-10 production from human memory CD4+ T cells. J Immunol 183 4475. PMID: 19734233.

Grodzki et al (2009) FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation. Exp Neurol 46 2539. PMID: 19540596.

Liu et al (2009) 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. Hypertens Res 32 846. PMID: 19662022.

Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011. PMID: 19547699.

Garcia et al (2008) Antigenic experience dictates functional role of glycogen synthase kinase-3 in human CD4+ T cell responses. J Immunol 181 8363. PMID: 19050253.

Nelson et al (2008) 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. J Neurochem 107 602. PMID: 18665913.

Chung et al (2007) IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol 194 77. PMID: 17592023.

Lin et al (2007) GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis. J Cell Sci 120 2935. PMID: 17666435.

Venkateswarlu et al (2007) PI-3-kinase-dependent membrane recruitment of centaurin-α2 is essential for its effect on ARF6-mediated actin cytoskeleton reorganisation. J Neurosci 120 792. PMID: 17284522.

Bianca et al (2006) Sphingosine 1-phosphate induces endothelial nitric-oxide synthase activation through phosphorylation in human corpus cavernosum. J Cell Biochem 316 703. PMID: 16234413.

O'Riordan et al (2006) Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors. J Neurosci 26 4870. PMID: 16672661.

Qiu et al (2006) Differential reelin-induced enhancement of NMDA and AMPA receptor activity in the adult hippocampus. Mol Cancer Ther 26 12943. PMID: 17167084.

Schlemper et al (2005) Mechanisms underlying the relaxation response induced by bradykinin in the epithelium-intact guinea-pig trachea in vitro. Br J Pharmacol 145 740. PMID: 15852038.

Searl and Silinsky (2005) LY 294002 inhibits adenosine receptor activation by a mechanism independent of effects on PI-3 kinase or casein kinase II. Purinergic Signal 1 389. PMID: 18404524.

Alonso-Magdalena et al Pancreatic insulin content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069. PMID: 18446233.

Do you know of a great paper that uses Wortmannin from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Wortmannin, supplier, Potent, inhibitors, inhibits, PLK1, PI, 3-kinase, irreversible, Polo-like, Kinases, PI3K, Mitosis, Phosphoinositide, SL2052, Tocris Bioscience, PI 3-kinase Inhibitor products

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