U-73122

U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.

Product Specifications

CAS Number

[112648-68-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ferroptosis; Lipoxygenase; Phospholipase

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/u-73122.html

Purity

99.79

Solubility

DMSO : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C=C1)N(CCCCCCN[C@H]2CC[C@@]3([H])[C@]4([H])CCC5=C(C=CC(OC)=C5)[C@@]4([H])CC[C@]23C)C1=O

Molecular Formula

C29H40N2O3

Molecular Weight

464.64

Precautions

H302, H315, H319, H335

References & Citations

[1]Smith RJ, et al. Receptor-coupled signal transduction in human polymorphonuclear neutrophils: effects of a novel inhibitor of phospholipase C-dependent processes on cell responsiveness. J Pharmacol Exp Ther. 1990 May;253 (2) :688-97.|[2]Bleasdale JE, et al. Selective inhibition of receptor-coupled phospholipase C-dependent processes in human platelets and polymorphonuclear neutrophils. J Pharmacol Exp Ther. 1990 Nov;255 (2) :756-68.|[3]Thompson AK, et al. The aminosteroid U-73122 inhibits muscarinic receptor sequestration and phosphoinositide hydrolysis in SK-N-SH neuroblastoma cells. A role for Gp in receptor compartmentation. J Biol Chem. 1991 Dec 15;266 (35) :23856-62.|[4]Peng T, et al. Disruption of phospholipase Cgamma1 signalling attenuates cardiac tumor necrosis factor-alpha expression and improves myocardial function during endotoxemia. Cardiovasc Res. 2008 Apr 1;78 (1) :90-7. Epub 2007 Dec 12.|[5]Frye CA, et al. In the ventral tegmental area, the membrane-mediated actions of progestins for lordosis of hormone-primed hamsters involve phospholipase C and protein kinase C. J Neuroendocrinol. 2007 Sep;19 (9) :717-24.|[6]Hörnig M, et al. Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416. Biochim Biophys Acta. 2012 Feb;1821 (2) :279-86.|[7]Xie W, et al. 3Beta-hydroxy-6-aza-cholestane and related analogues as phosphatidylinositol specific phospholipase C (PI-PLC) inhibitors with antitumor activity. Bioorg Med Chem. 2000 Apr;8 (4) :699-706.