For research use only.

Catalog No.S8011

37 publications

U73122 Chemical Structure

CAS No. 112648-68-7

U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).

Selleck's U73122 has been cited by 37 publications

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Biological Activity

Description U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).
PLC [1]
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 δ1 is neither activated nor inhibited. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Jurkat cells MV7GeY5kfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJJRmdG:vZYLhd4Uh[WO2aY\peJkhcW5iaIXtZY4hUnW{a3H0JINmdGy|IHL5JHRTSVBiYYPzZZktKEmFNUC9NE4zKM7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3M{W5Okc,OjRyNUO1PVY9N2F-

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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]


Solubility (25°C)

In vitro DMF 24 mg/mL warmed (51.65 mM)
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):
5% DMF+40% PEG300+5% Tween80+50% ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 112648-68-7
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID