MRL-SYKi

MRL-SYKi is a highly selective and potent chemical probe for spleen tyrosine kinase (SYK) . In live cell assays, it strongly binds to SYK gain-of-function (GoF) variants [SYK (S550Y), SYK (S550F), and SYK (P342T) ], with IC50 values of 2.1 nM, 14 nM, and 4.6 nM in digitonin-permeabilized cell experiments. MRL-SYKi effectively reduces catalytic activity, as shown in PhosphoSens SOX peptide assays, where the IC50 for SYK (S550F) is 63 nM and for SYK (P342T) is 95 nM. Additionally, it decreases phosphorylation levels at Y525/526 of SYK (S550Y) in SW480 cells. MRL-SYKi is useful for inflammation research.