4-アミノ-5-(4-フェノキシフェニル)-7-シクロペンチル-7H-ピロロ[2,3-d]ピリミジン

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

一般的な説明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 lck64-509 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) and in vivo (ED50 = 4 mg/kg in mice, ip.)