7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR

Lck Inhibitor is a cell-permeable ATP-competitive inhibitor of Lck.

A cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, 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 Lck_64-509 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) and in vivo (ED₅₀ = 4 mg/kg in mice, ip.)

Primary TargetLck?????? Y3