Lck Inhibitor

Lck Inhibitor is a cell-permeable pyrrolopyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of Lck (IC₅₀ at 5 μM ATP = < 1 nM, 2 nM, 70 nM, 1.57 μM and 1.98 μM for lck_64-509 Y₃₉4, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC₅₀ 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 (IC₅₀ = 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).