MRL-SYKi is a selective chemical probe targeting spleen tyrosine kinase (SYK). It demonstrates potent binding to gain-of-function variants of SYK, with IC50 values of 2.1 nM for SYK(S550Y), 14 nM for SYK(S550F), and 4.6 nM for SYK(P342T) in digitonin-permeabilized cell assays. MRL-SYKi effectively inhibits catalytic activity, achieving IC50 values of 63 nM and 95 nM for SYK(S550F) and SYK(P342T) respectively in phospho-specific assays. This compound is valuable for advancing research on inflammation and related signaling pathways.
MRL-SYKi is a selective chemical probe targeting spleen tyrosine kinase (SYK). It demonstrates potent binding to gain-of-function variants of SYK, with IC50 values of 2.1 nM for SYK(S550Y), 14 nM for SYK(S550F), and 4.6 nM for SYK(P342T) in digitonin-permeabilized cell assays. MRL-SYKi effectively inhibits catalytic activity, achieving IC50 values of 63 nM and 95 nM for SYK(S550F) and SYK(P342T) respectively in phospho-specific assays. This compound is valuable for advancing research on inflammation and related signaling pathways.
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