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Field of application
GSK143 is a highly potent, selective, orally efficacious Syk inhibitor with pIC50 of 7.5, >600-fold selective over ZAP-70; inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos cells with pIC50 of 7.1, and anti-IgM induced CD69 surface expression in primary B cells with pIC50 of 6.6; shows good efficacy in the rat Arthus model.
Sovleplenib is a highly potent inhibitor of spleen tyrosine kinase (Syk), derived from the innovative research disclosed in patent WO2012167733 A1. This compound demonstrates significant potential in modulating Syk-mediated signaling pathways, offering a promising therapeutic approach for conditions where Syk activity plays a critical role. Its development underscores the ongoing advancements in targeted kinase inhibition, providing a valuable tool for both research and potential clinical applications in immune-related and inflammatory diseases.
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
RDN2150 is a potent, selective and covalent ZAP-70 inhibitor with IC50 of 14.6 nM, shows no significant activity against Syk, covalently binds to the C346 residue of ZAP-70.
MTX-216 (MTX216) is a dual PI3K/EGFR inhibitor that blocks neurofibromin 1 loss of function (NF1LoF) melanoma cell growth in vitro and in vivo, suppresses the activity of SYK kinase with IC50 of 281 nM.