芦布妥林 T3689

Product Introduction
Bioactivity


英文名: Ruboxistaurin hydrochloride

描述: Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂，竞争性且可逆地抑制 PKCβI 和 PKCβII，IC50 值分别为 4.7 和 5.9 nM。

细胞实验: HUVECs are seeded into 96-well plates in low glucose DMEM with 10% FBS for 12 h. Afterwards, HUVECs are starved for 12 h and incubated with BSA (200 μg/ml), AGEs (200 μg/ml) and LY333531 (200 nM)+AGEs (200 μg/ml) for 48 h. Then, the medium is replaced with 0.5 mg/ml MTT and at 37 ?C in a 95% air/5% CO2 incubator for 4 h. Finally, the medium containing MTT is aspirated and replaced by dimethyl sulphoxide (DMSO). OD is measured with a Microplate spectrophotometer. AGEs:advanced glycation end products.(Only for Reference)

体外活性: 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[3].

体内活性: A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10.1 mg/mL (20 mM)


关键字: Ruboxistaurin Hydrochloride | LY 333531 | Ruboxistaurin hydrochloride | LY333531 | LY-333531 | LY-333531 Hydrochloride | LY 333531 Hydrochloride | Inhibitor | inhibit | LY333531 Hydrochloride | PKC | Protein kinase C

相关产品: DCP-LA | ZIP acetate(863987-12-6 free base) | Cercosporin | PKCβ inhibitor 1 | Darovasertib | TAT-SAMβA | VTX-27 | 20-Deoxyingenol 3-angelate | PKC-theta inhibitor hcl | NH125

相关库: Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Kinase Inhibitor Library | TGF-beta/Smad Compound Library | Bioactive Compound Library

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