7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
Lck Inhibitor is a cell-permeable ATP-competitive inhibitor of Lck.
Allgemeine Beschreibung
A cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, 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
394, Lckcd pY
394, 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 Lck
64-509 Y
394, 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 (IC
50<1-40 nM in Jurkat T cells) and
in vivo (ED
50 = 4 mg/kg in mice, ip.)
Biochem/physiol Actions
Primary TargetLck?????? Y3
7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte