192050-59-2

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].

PKC-βI: 4.7 nM (IC₅₀); PKC-βII: 5.9 nM (IC₅₀); PKCη: 52 nM (IC₅₀); PKCδ: 250 nM (IC₅₀); PKCγ: 300 nM (IC₅₀); PKCα: 360 nM (IC₅₀); PKCε: 600 nM (IC₅₀)

[1] Jirousek MR, et al. (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J Med Chem. 1996;39(14):2664-2671. DOI:10.1021/jm950588y
[2] Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. DOI:10.2165/00126839-200708030-00007
[3] Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells in vitro. J Diabetes Sci Technol. 2007 Nov;1(6):929-35. DOI:10.1177/193229680700100620
[4] Nonaka A, et al. PKC-beta inhibitor (LY333531) attenuates leukocyte entrapment in retinal microcirculation of diabetic rats. Invest Ophthalmol Vis Sci. 2000 Aug;41(9):2702-6. PMID:10937586