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Ruboxistaurin hydrochloride

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。

CAS号

169939-93-9

分子式

C28H28N4O3·HCl

主要靶点

PKC

仅限科研使用

Cat No : CM06020

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Synonyms

LY 333531 hydrochloride|LY333531 HCl|Ruboxistaurin|芦布妥林

验证数据展示

  • CAS No.: 169939-93-9

    Ruboxistaurin hydrochloride
    CAS#: 169939-93-9

产品信息

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).

CAS号 169939-93-9
分子式 C28H28N4O3·HCl
主要靶点 PKC
主要通路 表观遗传|细胞骨架
分子量 505.01
纯度 99.22%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LY 333531 hydrochloride|LY333531 HCl|Ruboxistaurin|芦布妥林

靶点活性

PKCβ1:4.7 nM|PKCη:0.052 μM|PKCγ:0.3 μM|PKCβ2:5.9 nM|PKCδ:0.25 μM

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.

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].

溶解度

DMSO:10.1 mg/mL (20 mM)

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)

参考文献

1.Jirousek MR, et al. J Med Chem. 1996, 39(14):2664-71.
2.Lei S, et al. Diabetes. 2013, 62(7):2318-28.
3.Wang SS, et al. Pharmazie. 2011, 66(11):881-7.

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