R-112 f Histone Demethylase 5-10 µM final concentration in

5-10 µM final concentration in various in vitro assays

is a potent protein kinase CK2 inhibitor

thereby inhibiting tumor cell migration

Meeting: 2011 ASCO Annual Meeting

In vivo it shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model

R-112 f Histone Demethylase 5-10 µM final concentration inR112 is a Syk inhibitor. R112 inhibited degranulation induced by anti IgE cross linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC(50)] = 353 nmol L) or basophils (histamine release, EC(50) = 280 nmol L), and by allergen (dust mite) in basophils (histamine release, EC(50) = 490 nmol L). R112 also blocked leukotriene C4 production and all proinflammatory cytokines tested. Subsequent molecular characterization