JTE-852 is a novel potent, selective, ATP-competitive Syk kinase inhibitor with IC50 of 1.25/1.28 nM for human/rat Syk, respectively.
JTE-852 is less potent for Lck (IC50=80 nM), and has IC50 of >300 nM against a kinase panel screenings;.
JTE-852 inhibits the kinase activity of Syk in an intracellular condition, suppresses the secretion of histamine, LTC4/D4/E4, TXA2, PGD2, and IL-13 from mast cells stimulated by IgE-crosslinking with IC50 of 40-100 nM.
JTE-852 attenuates IgG-mediated responses and signs in animal model of autoimmune diseases.
