Chemical Name: 6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one
Biological ActivityPotent inhibitor of lymphocyte specific kinase (Lck). IC50 values are 0.007, 0.021, 0.042 and 0.20 μM 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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