| 名称 | Ruboxistaurin hydrochloride |
| 描述 | Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src). |
| 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 | Ruboxistaurin strikingly decreases the chance of HUVEC survival and the effect of Ruboxistaurin 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, Ruboxistaurin reduces the ratio of Bcl-2/Bax. Ruboxistaurin 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 | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (108.91 mM), Sonication is recommended.
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| 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 | Darovasertib | α-Vitamin E |
| 相关库 | 经典已知活性库 | 激酶抑制剂库 | 药物功能重定位化合物库 | 抑制剂库 | 已知活性化合物库 | 人代谢物化合物库 | TGF-β/Smad靶点化合物库 |
United States
