Ranitidine is a histamine H2 receptor antagonist. It reverses histamine-induced relaxation of isolated rat uterine horn (pA2 = 6.9) as well as histamine-induced increases in contraction frequency in isolated guinea pig right atrium (pA2 = 7.2). Ranitidine (0.03-3 mg/kg, i.v.) inhibits histamine-and...

Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2...

GIT 27 is an orally active, isoxazole compound that exhibits various immunomodulatory properties both in vitro and in preclinical in vivo models of autoimmune diseases by inhibiting inflammatory antigen presentation. It has been shown to target macrophages, reducing the production of the proinflammatory mediators...

GDC-0879 is an inhibitor of B-RafV600E (IC50 = 0.13 nM for human recombinant enzyme). It is selective for B-RafV600E over a panel of 140 kinases at a concentration of 1 µM. GDC-0879 inhibits phosphorylation of ERK in MALME-3M cells (IC50 = 63 nM) as well as phosphorylation of MEK1 in COLO 205 and A375 cells that...