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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 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).
Burchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171. Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.
See how others have used Lck Inhibitor. Click on the entry to view the PubMed entry .
PMID: # 28250239 Singh, DK. et al. 2017. Reproduction. 153: 655-669.
PMID: # 24135919 Balbin, OA. et al. 2013. Nature communications. 4: 2617.
PMID: # 21487392 Cao, Y. et al. 2011. The EMBO journal. 30: 2083-93.
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