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Syk Inhibitor II, a cell-permeable pyrimidine-carboxamide compound that acts as a potent, selective, and ATP-competitive inhibitor of Syk (IC50 = 41 nM), while affecting PKCe, PKCbII, ZAP-70, Btk, and Itk only at much higher concentrations (IC50 = 5.1, 11, 11.2, 15.5, and 22.6μM, respectively). Inhibits FceRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and passive cutaneous anaphylaxis (PCA) reaction in mice in vivo (ID50 = 13.2 mg/kg, s.c.).
Hisamichi, H., et al. 2005. Bioorg. Med. Chem. 13, 4936.
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