R-112 f Histone Demethylase KB-R7943 mesylate

KB-R7943 mesylate

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

is an ethyl ester derivative of GSK-J1

5-10 µM final concentration in various in vitro assays

R-112 f Histone Demethylase KB-R7943 mesylateR112 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