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Inhibitor of PLC activation
Inhibits agonist induced phospholipase C (PLC) activation (IC50=1-2.1 µM) in human platelets. It also inhibits agonist induced down-regulation of muscarinic receptors in SK-N-SH neuroblastoma cells. It is a useful tool to investigate receptor-mediated PI turnover in signal transduction. It is a potent inhibitor of human neutrophil adhesion to biological surfaces as well as adhesion-dependent granule exocytosis and oxidative burst. Inhibits 5-lipoxygenase in vivo and in vitro (IC50 = 30nM for recombinant enzyme and 2.4µM for PMNL homogenates).
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Product Details
| Alternative Name |
1-(6-((17β-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione |
|---|---|
| Appearance |
white to off-white solid |
| CAS |
112648-68-7 |
| Couple Target |
Lipoxygenase, Phospholipase, PLC |
| Couple Type |
Inhibitor |
| Formula |
C29H40N2O3 |
| MW |
464.7 |
| Purity |
≥98% (HPLC) |
| Solubility |
Soluble in methylene chloride or chloroform. Slightly soluble in DMSO (2mg/ml) or 100% ethanol (1mg/ml), sparingly soluble in aqueous solutions. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. U73122 is only sparingly soluble in aqueous media. Therefore the compounds are delivered to cells either after dissolving in organic solvents or complexing with serum proteins. Serum albumin (1-10mg/ml).Dissolve a weighed amount of U-73122 in methylene chloride or chloroform. Dispense in aliquots sufficient for one experiment into suitable vessels. Evaporate solvent with nitrogen. Stock solutions in DMSO or ethanol are stable for 2 months when stored at -20°C. Preferably dissolve just before use. Use caution in reusing stored DMSO solutions. Discard solutions that have turned to a pink color, which indicates a loss of inhibitor activity. Dried aliquots prepared from chloroform solutions are stable for up to 1 month when stored at -20°C.Useful range of concentrations for U-73122 is 0.1 to 10μM. The appropriate concentration will depend upon the cell type, cell density, medium concentration (the maleimide moiety of U-73122 may react with thiol containing compounds) and the particular cell parameter that is being measured. |
|---|---|
| Long Term Storage |
Ambient |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- A non-canonical role for pyruvate kinase M2 as a functional modulator of Ca2+ signalling through IP3 receptors: Lavik, A. R., McColl, K. S., et al.; Biochim. Biophys. Acta Mol. Cell Res. 1869, 119206 (2022), Abstract
- Global analysis of osteosarcoma lipidomes reveal altered lipid profiles in metastatic versus nonmetastatic cells: Roy, J., Dibaeinia, P., et al.; J. Lipid Res. 60, 375 (2019), Abstract
- 1-Palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) attenuates gemcitabine-induced neutrophil extravasation: J. Jeong, et al.; Cell Biosci. 9, 4 (2019), Abstract — Full Text
- Effect of selective serotonin (5-HT)2B receptor agonist BW723C86 on epidermal growth factor/transforming growth factor-α receptor tyrosine kinase and ribosomal p70 S6 kinase activities in primary cultures of adult rat hepatocytes: K. Naito, et al.; Biol. Pharm. Bull. 42, 631 (2019), Application(s): used w. adult rat liver hepatocytes, Abstract — Full Text
- Constitutive IP3 signaling underlies the sensitivity of B-cell cancers to the Bcl-2/IP3 receptor disruptor BIRD-2: Bittremieux, M., La Rovere, R. M., et al.; Cell Death Differ. 26, 531 (2019), Abstract
- NLR members NLRC4 and NLRP3 mediate sterile inflammasome activation in microglia and astrocytes: Freeman, L., Guo, H., et al.; J. Exp. Med. 214, 1351 (2017), Abstract
- VLDL-activated cell signaling pathways that stimulate adrenal cell aldosterone production: Y.Y. Tsai, et al.; Mol. Cell. Endocrinol. 433, 138 (2016), Application(s): Cell culture, Abstract
- FGF9-induced changes in cellular redox status and HO-1 upregulation are FGFR-dependent and proceed through both ERK and AKT to induce CREB and Nrf2 activation: J.I. Chuang, et al.; Free Radic. Biol. Med. 89, 274 (2015), Application(s): Cell Culture, Abstract
- The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML: Obba, S., Hizir, Z., et al.; Autophagy 11, 1114 (2015), Abstract
- Serine-727 phosphorylation activates hypothalamic STAT-3 independently from tyrosine-705 phosphorylation: A. Breit, et al.; Mol. Endocrinol. 29, 445 (2015), Application(s): ELISA, Abstract — Full Text
- 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
- CXCL12 regulates platelet activation via the regulator of G-protein signaling 16: Z.A. Karim, et al.; Biochim. Biophys. Acta 1863, 314 (2015), Application(s): Cell culture, Abstract
- From blue light to clock genes in zebrafish ZEM-2S cells: Ramos, B. C., Moraes, M. N., et al.; PLoS One 9, e106252 (2014), Application(s): In Vitro, Abstract
- Activation of a TRP-like channel and intracellular Ca2+ dynamics during phospholipase-C-mediated cell death: Gonçalves, A. P., Cordeiro, J. M., et al.; J. Cell Sci. 127, 3817 (2014), Abstract
- Extracellular nucleotides inhibit oxalate transport by human intestinal Caco-2-BBe cells through PKC-δ activation: Amin, R., Sharma, S., et al.; Am. J. Physiol. Cell Physiol. 305, C78 (2013), Abstract
- FGF8 signaling is chemotactic for cardiac neural crest cells: Sato, A., Scholl, A. M., et al.; Dev. Biol. 354, 18 (2011), Abstract
- Regulation of constitutive cargo transport from the trans-Golgi network to plasma membrane by Golgi-localized G protein betagamma subunits: R. Irannejad & P.B. Wedegaertner; J. Biol. Chem. 285, 32393 (2010), Application(s): HeLa cells treatment, Abstract — Full Text
- Comparative Effects of the Endogenous Agonist Glucagon-Like Peptide-1 (GLP-1)-(7-36) Amide and the Small-Molecule Ago-Allosteric Agent Compound 2″ at the GLP-1 Receptor”””: K. Coopman, et al.; J. Pharmacol. Exp. Ther. 334, 795 (2010), Application(s): IP of human embryonic kidney cells, Abstract — Full Text
- The aminosteroid phospholipase C antagonist U-73122 (1-[6-[[17-beta-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrro le-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro: C. Feisst, et al.; Mol. Pharmacol. 67, 1751 (2005), Abstract
- U-73122: a potent inhibitor of human polymorphonuclear neutrophil adhesion on biological surfaces and adhesion-related effector functions: R.J. Smith, et al.; J. Pharmacol. Exp. Ther. 278, 320 (1996), Abstract
- U-73122, a phospholipase C antagonist, inhibits effects of endothelin-1 and parathyroid hormone on signal transduction in UMR-106 osteoblastic cells: A. Tatrai, et al.; Biochim. Biophys. Acta 1224, 575 (1994), Abstract
- A phospholipase C inhibitor, U-73122, blocks TSH-induced inositol trisphosphate production, Ca2+ increase and arachidonic acid release in FRTL-5 thyroid cells: X.D. Wang, et al.; Biochim. Biophys. Acta 1223, 101 (1994), Abstract
- Use of U-73122 as an Inhibitor of Phospholipase C-Dependent Processes: J.E. Bleasdale & S.K. Fisher; Neuroprotocols 3, 125 (1993), Full Text
- U73122 inhibits Ca2+ oscillations in response to cholecystokinin and carbachol but not to JMV-180 in rat pancreatic acinar cells: D.I. Yule, et al.; J. Biol. Chem. 267, 13830 (1992), Abstract
- U-73122, an aminosteroid phospholipase C antagonist, noncompetitively inhibits thyrotropin-releasing hormone effects in GH3 rat pituitary cells: R.C. Smallridge, et al.; Endocrinology 131, 1883 (1992), Abstract
- The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation: A.K. Thompson, et al.; J. Biol. Chem. 266, 23856 (1991), Abstract
- Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness: R.J. Smith, et al.; J. Pharmacol. Exp. Ther. 253, 688 (1990), Abstract
- Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils: J.E. Bleasdale, et al.; J. Pharmacol. Exp. Ther. 255, 756 (1990), Abstract
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