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PI3 kinase inhibitor
Potent and selective inhibitor of phosphatidyl-inositol 3-kinase. Active in purified preparations and cytosolic fractions(IC50 = 5nM) and is highly cell permeable. Inhibits fMLP induced PIP3 and superoxide anion production (IC50 = 50nM) in guinea pig neutrophils and blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Covalently binds to PI 3-kinase and is selective, inhibiting other kinases such as PI 4-kinase and myosin light chain kinase at concentrations 100-fold higher than that required for inhibition of PI 3-kinase. The half-life of wortmannin in culture media is quite short (8-13 minutes), care should be taken to account for this decomposition when planning experiments. Markedly potentiates the LPS-induced nitric oxide (NO) production from macrophages. Induces in vivo Alzheimer-like hyperphosphorylation in tau.
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Product Details
| Alternative Name |
KY 12420 |
|---|---|
| Appearance |
White to off-white solid. |
| CAS |
19545-26-7 |
| Couple Target |
PI3 kinase |
| Couple Type |
Inhibitor |
| Formula |
C23H24O8 |
| MI |
14: 10053 |
| MW |
428.4 |
| Purity |
≥98% (HPLC, TLC) |
| RTECS |
CB9641000 |
| Solubility |
Soluble in DMSO (50mg/ml), methanol (5mg/ml) or 100% ethanol (25mg/ml). |
| Source |
Isolated from Penicillium wortmannii |
| Technical Info / Product Notes |
Replacement for ADI-HPK-114. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Make solutions fresh immediately before use. DO NOT STORE SOLUTIONS. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Pseudorabies virus infection triggers pUL46-mediated phosphorylation of connexin-43 and closure of gap junctions to promote intercellular virus spread: Tishchenko, A., Romero, N., et al.; PLoS Pathog. 21, e1012895 (2025), Abstract
- Magnetic colloidal nanoformulations to remotely trigger mechanotransduction for osteogenic differentiation: M. Estévez, et al.; J. Colloid Interface Sci. 15, 664 (2024), Abstract
- Picolinafen exposure induces ROS accumulation and calcium depletion, leading to apoptosis in porcine embryonic trophectoderm and uterine luminal epithelial cells: W. Park, et al.; Theriogenology 201, 12 (2023), Abstract
- Sequestration of translation initiation factors in p62 condensates: A. Danieli, et al.; Cell Rep. 42, 113583 (2023), Abstract
- Defective quality control autophagy in Hyperhomocysteinemia promotes ER stress and consequent neuronal apoptosis through proteotoxicity: B. Kaur, et al.; Cell Commun. Signal. 21, 258 (2023), Abstract
- Transplantation of insulin-producing cells derived from human mesenchymal stromal/stem cells into diabetic humanized mice: M.A. Ghoneim, et al.; Stem Cell Res. Ther. 350, s13287 (2022), Abstract
- Exposure to fipronil induces cell cycle arrest, DNA damage, and apoptosis in porcine trophectoderm and endometrial epithelium, leading to implantation defects during early pregnancy: W. Park, et al.; Environ. Pollut. 291, 118234 (2021), Abstract
- Autophagy-Associated IL-15 Production Is Involved in the Pathogenesis of Leprosy Type 1 Reaction: B.J.A. Silva, et al.; Cells 10, 2215 (2021), Abstract
- Effects of Ipriflavone-Loaded Mesoporous Nanospheres on theDifferentiation of Endothelial Progenitor Cells and TheirModulation by Macrophages: L. Casarrubios, et al.; Nanomaterials 11, 1102 (2021), Abstract
- Acid sphingomyelinase promotes SGK1-dependent vascular calcification: T. Luong, et al.; Clin. Sci. 135, 515 (2021), Abstract — Full Text
- A temporal Ca 2+-desensitization of myosin light chain kinase in phasic smooth muscles induced by CaMKKß/PP2A pathways: T. Kitazawa, et al.; Am. J. Physiol. Cell Physiol. 321, C549 (2021), Abstract
- Matrix-assisted laser desorption/ionization mass spectrometry-guided visualization analysis of intestinal absorption of acylated anthocyanins in Sprague-Dawley rats: T.H. Hahm, et al.; Food Chem. 334, 127586 (2021), Abstract
- Actin Assembly around the Shigella-Containing Vacuole Promotes Successful Infection: Kühn, S., Bergqvist, J., et al.; Cell Rep. 31, 107638 (2020), Abstract
- A new form of actin assembly around the i>Shigella/i>-containing vacuole regulates its intracellular niche: Kühn, S., Bergqvist, J., et al.; bioRxiv , (2020)
- SGK1-dependent stimulation of vascular smooth muscle cell osteo-/chondrogenic transdifferentiation by interleukin-18: N. Schelski, et al.; Pflugers Arch. 471, 889 (2019), Abstract — Full Text
- Dual RXR motifs regulate nerve growth factor-mediated intracellular retention of the delta opioid receptor: D.J. Shiwarski, et al.; Mol. Biol. Cell 30, 680 (2019), Application(s): Treatment of PC12 cell cultures, Abstract — Full Text
- Additive effects of low concentrations of estradiol-17β and progesterone on nitric oxide production by human vascular endothelial cells through shared signaling pathways: Y. Pang & P. Thomas; J. Steroid Biochem. Mol. Biol. 165, 258 (2017), Application(s): Effects of steroids and inhibitors on NO production, Abstract
- Tumour-necrosis factor-α induces heparan sulfate 6-O-endosulfatase 1 (Sulf-1) expression in fibroblasts: A.S. Sikora, et al.; Int. J. Biochem. Cell Biol. 80, 57 (2016), Application(s): Treatment of MRC-5 cells , Abstract
- Neutrophils Discriminate between Lipopolysaccharides of Different Bacterial Sources and Selectively Release Neutrophil Extracellular Traps: E. Pieterse, et al.; Front. Immunol. 7, 484 (2016), Abstract — Full Text
- Is Wortmannin-Induced Reorganization of the trans-Golgi Network the Key to Explain Charasome Formation?: Foissner, I., Sommer, A., et al.; Front. Plant Sci. 7, 756 (2016), Abstract
- Proteomic analysis of novel targets associated with the enhancement of TrkA-induced SK-N-MC cancer cell death caused by NGF: Jung, E. J., Chung, K. H., et al.; Exp. Mol. Med. 48, e235 (2016), Abstract
- p130Cas scaffold protein regulates ErbB2 stability by altering breast cancer cell sensitivity to autophagy: Bisaro, B., Sciortino, M., et al.; Oncotarget 7, 4442 (2016), Abstract
- Antiviral potential of ERK/MAPK and PI3K/AKT/mTOR signaling modulation for Middle East respiratory syndrome coronavirus infection as identified by temporal kinome analysis: Kindrachuk, J., Ork, B., et al.; Antimicrob. Agents Chemother. 59, 1088 (2015), Abstract
- ATP1A1-mediated Src signaling inhibits coronavirus entry into host cells: Burkard, C., Verheije, M. H., et al.; J. Virol. 89, 4434 (2015), Abstract
- Activation of phosphatidylinositol 3-kinase β by the platelet collagen receptors integrin α2β1 and GPVI: The role of Pyk2 and c-Cbl: D. Manganaro, et al.; Biochim. Biophys. Acta 1853, 1879 (2015), Application(s): Cell Culture, Abstract
- Molecular Analysis and Localization of CaARA7 a Conventional RAB5 GTPase from Characean Algae: Hoepflinger, M. C., Geretschlaeger, A., et al.; Traffic 16, 534 (2015), Abstract
- African swine fever virus infects macrophages, the natural host cells, via clathrin- and cholesterol-dependent endocytosis: I. Galindo, et al.; Virus Res. 200, 45 (2015), Application(s): Cell Culture, Abstract
- Role for Artemis nuclease in the repair of radiation-induced DNA double strand breaks by alternative end joining: M. Moscariello, et al.; DNA Repair (Amst.) 31, 29 (2015), Application(s): Cell Culture, Abstract
- Wnt/β-catenin signaling modulates human airway sensitization induced by β2-adrenoceptor stimulation: Faisy, C., Grassin-Delyle, S., et al.; PLoS One 9, e111350 (2014), Abstract
- Molecular and biochemical analysis of the first ARA6 homologue, a RAB5 GTPase, from green algae: Hoepflinger, M. C., Geretschlaeger, A., et al.; J. Exp. Bot. 64, 5553 (2013), Abstract
- IRAK4 turns IL-10+ phospho-FOXO+ monocytes into pro-inflammatory cells by suppression of protein kinase B: Over, B., Ziegler, S., et al.; Eur. J. Immunol. 43, 1630 (2013), Abstract
- Cornel Iridoid Glycoside Attenuates Tau Hyperphosphorylation by Inhibition of PP2A Demethylation: C.C. Yang, et al.; Evid. Based Complement. Alternat. Med. 2013, 108486 (2013), Application(s): IC, WB, Abstract — Full Text
- Retromer subunits VPS35A and VPS29 mediate prevacuolar compartment (PVC) function in Arabidopsis: Nodzynski, T., Feraru, M. I., et al.; Mol. Plant 6, 1849 (2013), Abstract
- Insulin stimulates translocation of human GLUT4 to the membrane in fat bodies of transgenic Drosophila melanogaster: G. Crivat, et al.; PloS One 8, e77953 (2013), Application(s): Fluorescence Microscopy, Abstract — Full Text
- TR3 modulates platinum resistance in ovarian cancer: A.J. Wilson, et al.; Cancer Res. 73, 4758 (2013), Application(s): WB, IF, IHC, Abstract — Full Text
- bis-Dehydroxy-Curcumin Triggers Mitochondrial-Associated Cell Death in Human Colon Cancer Cells through ER-Stress Induced Autophagy: V. Basile, et al.; PloS One 8, e53664 (2013), Application(s): WB, IF, PCR, Abstract — Full Text
- Internalized gap junctions are degraded by autophagy: Fong, J. T., Kells, R. M., et al.; Autophagy 8, 794 (2012), Abstract
- Wortmannin reduces insulin signaling and death in seizure-prone Pcmt1-/- mice: MacKay, K. B., Lowenson, J. D., et al.; PLoS One 7, e46719 (2012), Abstract
- Anaphylaxis to cow’s milk formula containing short-chain galacto-oligosaccharide: W.C. Chiang, et al.; J. Allergy Clin. Immunol. 130, 1361 (2012), Application(s): Flow Cytometry, Abstract
- Enhanced contractility and myosin phosphorylation induced by Ca2+-independent MLCK activity in hypertensive rats: Y.E. Cho, et al.; Cardiovasc. Res. 91, 162 (2011), Application(s): IF, Abstract — Full Text
- Rho-kinase inhibition attenuates calcium-induced contraction in β-escin but not Triton X-100 permeabilized rabbit femoral artery: Clelland, L. J., Browne, B. M., et al.; J. Muscle Res. Cell Motil. 32, 77 (2011), Abstract
- Stimulus-specific blockade of nitric oxide-mediated dilatation by asymmetric dimethylarginine (ADMA) and monomethylarginine (L-NMMA) in rat aorta and carotid artery: M.J. Al-Zobaidy, et al.; Eur. J. Pharmacol. 673, 78 (2011), Application(s): Wortmannin effect on acetylcholine-induced relaxation of cardiac tissue, Abstract
- Induction of steroid sulfatase expression by tumor necrosis factor-α through phosphatidylinositol 3-kinase/Akt signaling pathway in PC-3 human prostate cancer cells: B.Y. Suh, et al.; Exp. Mol. Med. 43, 646 (2011), Application(s): WB, IF, PCR, Abstract — Full Text
- Leukotrienes target F-actin/cofilin-1 to enhance alveolar macrophage anti-fungal activity: Morato-Marques, M., Campos, M. R., et al.; J. Biol. Chem. 286, 28902 (2011), Abstract
- The AP-3 β adaptin mediates the biogenesis and function of lytic vacuoles in Arabidopsis: Feraru, E., Paciorek, T., et al.; Plant Cell 22, 2812 (2010), Abstract
- Protective actions of epoxyeicosatrienoic acid: dual targeting of cardiovascular PI3K and KATP channels: Bodiga, S., Zhang, R., et al.; J. Mol. Cell. Cardiol. 46, 978 (2009), Abstract
- A double hit to kill tumor and endothelial cells by TRAIL and antiangiogenic 3TSR: Ren, B., Song, K., et al.; Cancer Res. 69, 3856 (2009), Abstract
- Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity: Maira, S. M., Stauffer, F., et al.; Mol. Cancer Ther. 7, 1851 (2008), Abstract
- Chemistry and biology of wortmannin: P. Wipf & R.J. Halter; Org. Biomol. Chem. 3, 2053 (2005), Abstract
- ANG II activates effectors of mTOR via PI3-K signaling in human coronary smooth muscle cells: Hafizi, S., Wang, X., et al.; Am. J. Physiol. Heart Circ. Physiol. 287, H1232 (2004), Abstract
- Use of high-performance liquid chromatography to characterize the rapid decomposition of wortmannin in tissue culture media:: J.L. Holleran, et al.; Anal. Biochem. 323, 19 (2003), Abstract
- Alzheimer-like tau phosphorylation induced by wortmannin in vivo and its attenuation by melatonin: S.J. Liu & J.Z. Wang; Acta Pharmacol. Sin. 23, 183 (2002), Abstract
- Reduction of Abeta accumulation in the Tg2576 animal model of Alzheimer’s disease after oral administration of the phosphatidyl-inositol kinase inhibitor wortmannin: Haugabook, S. J., Le, T., et al.; FASEB J. 15, 16 (2001), Abstract
- Phosphatidylinositol 3-kinase-dependent activation of trypsinogen modulates the severity of acute pancreatitis: Singh, V. P., Saluja, A. K., et al.; J. Clin. Invest. 108, 1387 (2001), Abstract
- Wortmannin, a specific inhibitor of phosphatidylinositol-3-kinase, enhances LPS-induced NO production from murine peritoneal macrophages: Y.C. Park, et al.; BBRC 240, 692 (1997), Abstract
- The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes: E.F. Blommaart, et al.; Eur. J. Biochem. 243, 240 (1997), Abstract
- Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction: M.P. Wymann, et al.; Mol. Cell. Biol. 16, 1722 (1996), Abstract
- Inhibitory effect of wortmannin on phosphatidylinositol 3-kinase-mediated cellular events: O. Hazeki, et al.; J. Lipid Mediat. Cell Signal. 14, 259 (1996), Abstract
- Wortmannin, a specific phosphatidylinositol 3-kinase inhibitor, inhibits adipocytic differentiation of 3T3-L1 cells: K. Tomiyama, et al.; BBRC 212, 263 (1995), Abstract
- Wortmannin as a unique probe for an intracellular signalling protein, phosphoinositide 3-kinase: M. Ui, et al.; TIBS 20, 303 (1995), (Review), Abstract
- Wortmannin, a specific inhibitor of phosphatidylinositol-3 kinase, blocks osteoclastic bone resorption: I. Nakamura, et al.; FEBS Lett. 361, 79 (1995), Abstract
- Wortmannin inhibits carcinogen-stimulated phosphorylation of ethanolamine and choline: Z. Kiss & M. Tomono; FEBS Lett. 358, 243 (1995), Abstract
- Wortmannin inhibits insulin-stimulated but not contraction-stimulated glucose transport activity in skeletal muscle: A.D. Lee, et al.; FEBS Lett. 361, 51 (1995), Abstract
- Essential role of phosphatidylinositol 3-kinase in insulin-induced glucose transport and antilipolysis in rat adipocytes. Studies with a selective inhibitor wortmannin: T. Okada, et al.; J. Biol. Chem. 269, 3568 (1994), Abstract
- Effects of wortmannin on increased glucose transport by insulin and norepinephrine in primary culture of brown adipocytes: Y. Shimizu & T. Shimazu; BBRC 202, 660 (1994), Abstract
- Blockage of chemotactic peptide-induced stimulation of neutrophils by wortmannin as a result of selective inhibition of phosphatidylinositol 3-kinase: T. Okada, et al.; J. Biol. Chem. 269, 3563 (1994), Abstract
- A comparison of demethoxyviridin and wortmannin as inhibitors of phosphatidylinositol 3-kinase: R. Woscholski, et al.; FEBS Lett. 342, 109 (1994), Abstract
- Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses: A. Arcaro & M.P. Wyman; Biochem. J. 296, 297 (1993), Abstract
- Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells: H. Yano, et al.; J. Biol. Chem. 268, 25846 (1993), Abstract — Full Text
- Wortmannin, a microbial product inhibitor of myosin light chain kinase: S. Nakanishi, et al.; J. Biol. Chem. 267, 2157 (1992), Abstract — Full Text
- Inhibition of IgE-mediated histamine release by myosin light chain kinase inhibitors: S. Kitani, et al.; BBRC 183, 48 (1992), Abstract
- Demethoxyviridin and wortmannin block phospholipase C and D activation in the human neutrophil: R.W. Bonser, et al.; Br. J. Pharmacol. 103, 1237 (1991), Abstract
- Activation of human neutrophil phospholipase D by three separable mechanisms: S.I. Reinhold, et al.; FASEB J. 4, 208 (1990), Abstract
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