ER-27319 (maleate)

ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC₅₀ of 10 μM and can be used for study in allergic diseases^{[1] [2]} . IC50 & Target:10 μM (Syk) in human and rat mast cells^[1] In Vitro: ER-27319 (maleate) (24 h) inhibits antigen-induced generation of inositol phosphates, release of arachidonic acid, and secretion of histamine and tumor necrosis factor α in RBL-2H3 cells, rat peritoneal and human cultured mast cells, and with IC₅₀ value of 10 μM, approximately^[1].
ER-27319 (maleate) (10-30 μM, 10 min) selectivity inhibits the tyrosine phosphorylation of SYK induced by the phosphorylated immunoreceptor tyrosine-based activation motif of the FcεRI γ in RBL-2H3 cells^[1].
ER-27319 (maleate) (up to 100 μM, 60 min) does not inhibit the the tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation in the Jurkat cells^[1].
ER-27319 (maleate) (100 μM, 10 min) inhibits the tyrosine phosphorylation of two proteins (38, 70 kD) and decreases the tyrosine phosphorylation of the other two proteins (62, 80 kD) in anti-IgG stimulation Canine cutaneous mastocytoma-derived cells^[2].