Chemical Name:10-(3-Aminopropyl)-3,4-dimethyl-9(10H)-acridinone
maleate
Biological Activity:
Selective
inhibitor of Syk kinase. Inhibits tyrosine phosphorylation of Syk initiated by
the engagement of FceRI in rat and human mast cells. Results in the abrogation of
degranulation, TNF-α production (IC50 = 10 μM) and other related signalling
events.
Moriya et al (1997) ER-27319, an acridone-related
compound, inhibits release of antigen-induced allergic mediators from mast
cells by selective inhibition of Fcε receptor I-mediated activation of Syk. Proc.Natl.Acad.Sci.USA 94 12539.
Luskova and Draber (2004) Modulation of the Fcepsilon receptor I
signaling by tyrosine kinase inhibitors: search for therapeutic targets of
inflammatory and allergy diseases. Curr.Pharm.Des. 10 1727.