Ruboxistaurin hydrochloride(又名鲁伯斯塔盐酸盐, LY333531 hydrochloride, Ruboxistaurin (LY333531) HCl, Ruboxistaurin HCl)是一种选择性的,ATP-竞争性的PKCβ抑制剂,可逆地抑制PKCβ1和PKCβ2,其IC50分别为4.7 nM和5.9 nM。Ruboxistaurin hydrochloride对PKCη (IC50=52 nM),PKCα (IC50=360 nM),PKCγ (IC50=300 nM),PKCδ (IC50=250 nM)表现为较小的抑制作用,对PKCζ (IC50>100 μM)几乎没有影响。
参考文献
[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 Jul 5;39(14):2664-71.
[2] 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.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。