Ruboxistaurin (mesylate)

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^[1][2][3][4]. IC50 & Target:IC50:4.7 nM and 5.9 nM (PKCβ), K_i: 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^[1].
Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC₅₀ values of 6.2 and 0.32 μM, respectively^[1].
Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions^[3]. 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^[4].