Syk Inhibitor II (dihydrochloride)

Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect^[1]. IC50 & Target:IC₅₀:41 nM (Syk)^[1] In Vitro:Syk Inhibitor II (compound 9a) dihydrochloride shows less potent against PKCε, PKCβ2, ZAP-70, Btk, and Itk with IC₅₀ values of 5.1 µM, 11 µM, 11.2 µM, 15.5 µM, and 22.6 µM, respectively^[1]. In Vivo:Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID₅₀ value of 13.2 mg/kg^[1].