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Submit ReviewWortmannin 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).
分子量 | 428.44 |
公式 | C23H24O8 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 19545-26-7 |
PubChem ID | 3003565 |
InChI Key | QDLHCMPXEPAAMD-ZGSWIPFCSA-N |
Smiles | O=C(C4=CO5)O[C@H](COC)[C@@]1(C)C4=C5C(C2=C1[C@H](OC(C)=O)C[C@@]3(C)C2CCC3=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 21.42 | 50 |
以下数据基于产品分子量 428.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.67 mL | 23.34 mL | 46.68 mL |
2.5 mM | 0.93 mL | 4.67 mL | 9.34 mL |
5 mM | 0.47 mL | 2.33 mL | 4.67 mL |
25 mM | 0.09 mL | 0.47 mL | 0.93 mL |
参考文献是支持产品生物活性的出版物。
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
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
Powis et al (1994) Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Res. 54 2419 PMID: 8162590
Schultz et al (1995) In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor wortmannin. Anticancer Res. 15 1135 PMID: 7653991
If you know of a relevant reference for Wortmannin, please let us know.
关键词: Wortmannin, Wortmannin supplier, Potent, inhibitors, inhibits, PLK1, PI, 3-kinase, irreversible, Polo-like, Kinases, PI3K, Mitosis, Phosphoinositide, SL2052, vps34, autophagy, SL-2052, Inositol, Lipids, 3-Kinase, Kinase, Autophagy, 1232, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Wortmannin 的部分引用包括:
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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
Accardi et al (2015) α6-Containing GABAA Receptors Are the Principal Mediators of Inhibitory Synapse Strengthening by Ins in Cerebellar Granule Cells. J Neurosci 35 9676 PMID: 26134650
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
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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
Grassin-Delyle et al (2013) The expression and relaxant effect of bitter taste receptors in human bronchi. Respir Res 14 134 PMID: 24266887
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
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
Roselli et al (2011) CDK5 is essential for soluble amyloid β-induced degradation of GKAP and remodeling of the synaptic actin cytoskeleton. PLoS One 6 e23097 PMID: 21829588
Sidhar and Giri (2017) Induction of Bex genes by curcumin is associated with apoptosis and activation of p53 in N2a neuroblastoma cells. Sci Rep 7 41420 PMID: 28145533
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
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
Martín-Segura et al (2019) Age-associated cholesterol reduction triggers brain Ins. resistance by facilitating ligand-independent receptor activation and pathway desensitization. Aging Cell 18 e12932 PMID: 30884121
Wijerathne et al (2019) Onion peel extract and its constituent, quercetin inhibits human Slo3 in a pH and calcium dependent manner. Korean J Physiol Pharmacol 23 381 PMID: 31496875
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Huang et al (2010) Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor. J Neurosci 30 6080 PMID: 20427666
Heberle et al (2019) The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner. Life Sci Alliance 2 PMID: 30923191
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
Ruisanchez et al (2014) Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J 28 880 PMID: 24249637
Nazarians-Armavil et al (2013) Cellular Ins resistance disrupts leptin-mediated control of neuronal signaling and transcription. Mol Endocrinol 27 990 PMID: 23579487
Faria et al (2013) Melatonin acts through MT1/MT2 receptors to activate hypothalamic Akt and suppress hepatic gluconeogenesis in rats. Am J Physiol Endocrinol Metab 305 E230 PMID: 23695212
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
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
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Ahmed (2016) Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. Physiological Reports 4 e13069 PMID: 28039410
Yao et al (2015) Endothelial Rac1 is essential for hematogenous metastasis to the lung. Sci Rep 6 17501 PMID: 25991673
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
Sahay et al (2015) The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer. PLoS One 6 20604 PMID: 26098771
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Zhang et al (2018) Integrin CD11b negatively regulates Mincle-induced signaling via the Lyn-SIRPα-SHP1 complex. Exp Mol Med 50 e439 PMID: 29400702
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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
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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
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
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
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
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
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Rojas et al (2007) Protein kinase C dependent inhibition of the heteromeric Kir4.1-Kir5.1 channel. Biochim Biophys Acta 1768 2030 PMID: 17585871
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
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