Potent inhibitor of lymphocyte specific kinase (Lck). IC50
values are 0.007, 0.021, 0.042 and 0.20 μ
M for Lck, Lyn, Src and Syk kinases respectively. Displays >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Inhibits T cell proliferation in vitro
and inhibits arthritis in two in vivo
models. Orally active.
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All Tocris products are intended for laboratory research use only.
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory
Martin et al.