Ruboxistaurin hydrochloride NEW
| Price | $65 | $94 | $159 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: Ruboxistaurin hydrochloride | CAS No.: 169939-93-9 |
| Purity: 99.22% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | 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). |
| 細(xì)胞實驗 | 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) |
| 體外活性 | 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]. |
| 體內(nèi)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. |
| 存儲條件 | 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. |
| 關(guān)鍵字 | Ruboxistaurin Hydrochloride | LY 333531 | Ruboxistaurin hydrochloride | LY333531 | LY-333531 | LY-333531 Hydrochloride | LY 333531 Hydrochloride | Inhibitor | inhibit | LY333531 Hydrochloride | PKC | Protein kinase C |
| 相關(guān)產(chǎn)品 | Darovasertib | α-Vitamin E |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 人代謝物化合物庫 | TGF-β/Smad靶點化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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