U73122
Catalog No.S8011
Molecular Weight(MW): 464.64
U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN.
6 Customer Reviews
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Effect of U73122 and XC on TFEB phosphorylation
Cell Res, 2017, 27(6):748-763. U73122 purchased from Selleck.
E）Average fluorescence curve of H9c2(2-1) cells treated or not with U-73122 (10 μM).
Virus Genes, 2016, 53(2):179-189. U73122 purchased from Selleck.
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Downstream signaling of FGFR1 is required for neuritin-mediated axonal branching. A, U0126 (10 μM), a MEK1/2 inhibitor, LY294002 (20 μM), a PI3K inhibitor, or U73122 (2 μM), a PLC inhibitor, was applied to rat granule neurons expressing EGFP or expressing EGFP and neuritin at DIV 1. Neurons were fixed and imaged at DIV 4. Representative neurons expressing neuritin are shown. Scale bar, 50 μm. B, Quantification of the number of primary branches per 100 μm of axon (control vs neuritin, DMSO: p<0.001; U0126: p=0.222; LY294002: p=0.717; and U73122: p=0.001;DMSO vs each reagent in control, U0126: p=0.693; LY294002: p=0.016; and U73122: p=0.562) and the average length of primary branches (control vs neuritin, DMSO: p<0.001; U0126: p=0.411; LY294002: p=0.395; and U73122: p=0.099; DMSO vs each reagent in control, U0126: p=0.377; LY294002: p=0.002; and U73122: p=0.881) from three or four independent experiments with n 30 for each. Control versus neuritin: ***p<0.005 (one-way ANOVA for each reagent). n.s., Not significant. DMSO versus each reagent: #p<0.05 (a one-way ANOVA followed by Tukey’s post-test for the control). ###p<0.005 (a one-way ANOVA followed by Tukey’s post-test for the control). N, Not significant, compared with DMSO.
J Neurosci, 2016, 36(16):4534-48.. U73122 purchased from Selleck.
A-hBD-2 treatment increased the secretion of pro- and anti-inflammatory cytokines and chemokines and the PLC signaling pathway involved in this process. (a) HaCaT cells were separately incubated with vehicle, hBD-2, A-hBD-2, or A-hBD-2 and U73122 for 6 h, and the gene expression of proand anti-inflammatory cytokines and chemokines in HaCaT cells was detected using RT-PCR. (b) HaCaT cells were separately incubated with vehicle, hBD-2, A-hBD-2, or A-hBD-2 and U73122 for 48 h, and the production of pro- and anti-inflammatory cytokines and chemokines in HaCaT cells was detected using ELISA. All experiments were performed in triplicate. Data are expressed as the mean ± SD. *P<0.05, **P<0.01, ***P<0.001, ****P<0.0001
Cell Physiol Biochem, 2018, 51(2):647-663. U73122 purchased from Selleck.
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Effects of intracellular signaling pathway inhibitors on GnRH-stimulated Gh release. The primary cultured pituitary cells of intersexual ricefield eels were pre-incubated for 24 h before being treated with 100 nM of GnRH1 (A) or GnRH3 (B) in the presence or absence of inhibitors Rp-cAMPS (50 μM), U73122 (10 μM), GF109203X (20 μM), Xestospongin C (1 μM), or Nifedipine (10 μM) for 4 h, respectively. After drug treatment, culture medium was harvested for measurement of Gh release by competitive ELISA. Data were expressed as fold change relative to the vehicle control. Bars represent means ± SEM (n = 3). *P < 0.05 vs.the vehicle control.
Front Endocrinol, 2018, doi:10.3389/fendo.2018.00721. U73122 purchased from Selleck.
The Src/PLC/PKC signaling pathway may trigger integrin endocytosis. (A) Representative picture of CHO cells labeling with FITCconjucted- CD41 spreading on immobilized Fg for 90 minutes after treated with the Src inhibitor PP2, FAK inhibitor PF-573228, Syk inhibitor Piceatannol, PLC inhibitor U73122, PKC inhibitor Ro 31-8220, microtubule inhibitor Taxol or actin polymerization inhibitor Cytochalasin D. Images were taken under oil immersion with magnification × 100. Scale bar, 20 μm.
Platelets, 2018, 29(6):610-621. U73122 purchased from Selleck.
Purity & Quality Control
Choose Selective Phospholipase (e.g. PLA) Inhibitors
Biological Activity
| Description | U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. | ||||||||||||||||
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| Targets |
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| In vitro |
U73122 significantly inhibits aggregation of human platelets induced by a variety of agonists, including collagen, thrombin, ADP, arachidonic acid, with IC50 of 1-5 μM. U-73122 (10 μM) inhibits the production of IP3 and the subsequent rapid increase in cytosolic Ca2+ induced by either thrombin or U-46619 through inhibiting hydrolysis of phosphatidyl[3H]inositol and phosphatldyl[3H]inosito1 4,5-bisphosphate catalyzed by a soluble fraction from platelets (Ki=9 and 40 μM, respectively). U-73122 inhibits thromboxane B production induced by collagen through inhibiting receptor-coupled mobilization of arachidonic acid. U73122 inhibits also FMLP-induced aggregation of human polymorphonuclear neutrophils and the associated production of IP3 and diacylglycerol. [1] U-73122 causes a concentration-dependent inhibition of C5a, FMLP, PAF and LTB4-induced MPO and B12-BP release from cyto-chalasin B-treated PMNs. The IC50 values are 60 (FMLP), 110 (LTB4), 115 (C5a) and 120 (PAF) nM for MPO release; and 105 (FMLP), 110 (LTB4), 120 (C5a) and 140 (PAY) nM for B12-BP release. U-73122 is also a potent inhibitor of superoxide anion production by cytochalasin B-treated PMNs activated with either C5a or FMLP with IC50 of 160 and 300 nM, respectively. U-73122 causes suppression of the rise in [Ca2+]i, IP3 production and DAG production in FMLP-stimulated PMNs with IC50 of 500 nM, 2 μM, and 2 μM, respectively. 3 μM U-73122 causes 100% inhibition of FMLP-induced GTPase activity. U-73122 causes a concentration-dependent inhibition of the FMLP-evoked association of PKC with the extractable particulate fraction of PMNs, but not a soluble preparation of PMN PKC. [2] U73122 significantly inhibits recombinant human PLC-β2, with an IC50 of ~6 μM. U73122 has little effect on PLC-β1, PLC-β3, or PLC-β4. U73122 reduces interleukin-8 and leukotriene B4-induced Ca2+ flux and chemotaxis in human neutrophils with IC50 of ~6 μM and ~5 μM, respectively. [3] 1 μM U73122 blocks bradykinin (BK)-induced increases in the intracellular free Ca2+ concentration in undifferentiated NG108-15 cell. The IC50 for a 20-min exposure is approximately 200 nM. 1 μM U73122 produces a small but significant increase in [Ca2+]i which results from Ca 2+ release from an intracellular store. In differentiated NG108-15 cells U73122 blocks completely depolarization-induced Ca2+ influx. In contrast, in DRG neurons U73122 inhibits only slightly voltage-sensitive Ca2+ channels. [4] U73122 is a relatively specific inhibitor of G-protein-mediated phospholipase C activation in pancreatic acini. U73122 inhibits phosphatidylinositol (PI) hydrolysis on stimulation with either cholecystokinin (by 81%) or carbachol (by 73%) at a maximal effect concentration of 10 μM. U73122 (10 μM) inhibits the increases in [Ca2+]i stimulated by high concentrations of secretagogues in fura-2-loaded acini. U73122 also inhibits the [Ca2+]i signal generated by directly stimulating G-proteins with sodium fluoride. U73122 rapidly inhibits the oscillating [Ca2+]i signal elicited by low concentrations of cholecystokinin or carbachol. [5] U73122 increases the activity of hPLCβ3 in a concentration-and time-dependent manner in a cell-free micellar system, with up to an 8-fold increase in enzyme activity and a EC50 of 13.6 μM. Activation of hPLCβ3 by U73122 requires covalent modification of cysteines. U73122 (10 μM) also activates hPLCγ1(>10-fold) and hPLCβ2(~2-fold); PLC β1 is neither activated nor inhibited. [6] |
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| Cell Data |
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| In vivo | U73122 (30 mg/kg i.p.) blocks swelling of rats hind paw by 65 and 80% at 1 and 3 h postcarrageenan challenge. U73122 (0.1 mg/mL) inhibits carrageenan-induced macrophage and lymphocyte accumulation into subcutaneous chambers in dogs by 65 and 74%, respectively. U73122 (30 mg/kg i.p.) totally inhibits the LPS-induced increase in macrophage and lymphocyte infiltration and prostaglandin E2 production (by 80%) in a mouse peritonitis model, and inhibits and 12- O-tetradecanoyl-phorbol-13-acetate-induced ear edema in mice. [3] |
Protocol
Solubility (25°C)
| In vitro | DMF | 24 mg/mL warmed (51.65 mM) |
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| DMSO | 0.01 mg/mL warmed (0.02 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% Tween 80+saline For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 464.64 |
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| Formula | C29H40N2O3 |
| CAS No. | 112648-68-7 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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