Description
Lck Inhibitor is a cell-permeable pyrrolopyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of Lck (IC:50:at 5 µM ATP = < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck:64-509:Y:39:4, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC:50:at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC:50:= 3.2 µM, > 33 µM, > 50 µM and > 50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells)