MRL-SYKi is a chemical probe with high selectivity and potent activity against spleen tyrosine kinase (SYK). MRL-SYKi potently binds to SYK gain-of-function (GoF) variants (SYK(S550Y), SYK(S550F), and SYK(P342T)) in intact live cells, with IC50 values of 2.1 nM, 14 nM, and 4.6 nM respectively in digitonin-permeabilized cell assays. MRL-SYKi effectively reduces catalytic activity (IC50 = 63 nM for SYK(S550F) and 95 nM for SYK(P342T) in PhosphoSens SOX peptide assays). MRL-SYKi can decrease the phosphorylation level of SYK(S550Y) at Y525/526 in SW480 cells. MRL-SYKi can be used for the study of inflammation[1].
Molecular Weight:
452.57
Purity:
99.9
CAS Number:
[1312534-69-2]
Formula:
C24H28N4O3S
Target:
Syk
Application Notes:
MCE Product type: Reference compound
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