Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes[2].IC50 & Target:IC50:4.7 nM and 5.9 nM (PKCβ), Ki: 2 nM (PKCβ)sup>[1]In Vitro: Ruboxistaurin mesylate inhibits PKC isozymes with IC50 values of 0.36, 0.0047, 0.0059, 0.30, 0.25, 0.60 and 0.052 μM for PKCα, PKCβI, PKCβII, PKCγ, PKCδ, PKCε and PKCη, respectively.Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC50 values of 6.2 and 0.32 μM, respectively.Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions.In Vivo: Ruboxistaurin mesylate (0.1, 1.0 and 10.0 mg/kg; oral administration, once daily for 4 weeks) decreases the increasing of leukocyte entrapment in the retinal microcirculation during the early diabetes period.