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Ruboxistaurin hydrochloride
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产品介绍
产品介绍
产品信息
抗原名称
PKCβ1,PKCβ2,PKCγ,PKCδ,PKCη
商品描述
Ruboxistaurin hydrochloride is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
分子量
505.10
纯度
≥98%
可溶性
DMSO : 10.1 mg/mL (20 mM)
外观
red to orange powder
IC50
PKC beta II : IC50 = 5.9 nM; PKC beta I: IC50 = 4.7 nM
In vitro(体外研究)
LY333531 strikingly decreases the chance of HUVEC survival and the effect of LY333531 on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, LY333531 reduces the ratio of Bcl-2/Bax. LY333531 can further prompt AGEs-induced endothelial cells apoptosis. The increased expression of Bax, Bad and decreased expression of Bcl-2 and Bcl-2/Bax ratio are associated with the apoptotic process.
In vivo(体内研究)
LY333531 treatment (for a duration of 4 weeks) prevents excessive PKCb2 activation and attenuates cardiac diastolic dysfunction in rats with streptozotocin-induced diabetes. LY333531 suppresses the decreased expression of myocardial NO, Cav-3, phosphorylated (p)-Akt, and p-eNOS and also mitigates the augmentation of O2-, nitrotyrosine, Cav-1, and iNOS expression.
背景
别名
鲁伯斯塔盐酸盐；LY 333531 hydrochloride
分子式
C28H28N403•HCl
CAS号
169939-93-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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