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Salubrinal

现货
Catalog No.
B2025
eIF2α抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,800.00
现货
10mg
¥ 1,050.00
现货
25mg
¥ 2,090.00
现货

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Background

IC50: A cell-permeable and selective inhibitor of eIF2α dephosphorylation with an IC50 of 15 M.

The eukaryotic translation initiation factor 2 subunit α (eIF2α) is crucial in protein synthesis. eIF2α phosphorylation played an important role in protecting cells from apoptosis. Salubrinal selectively suppresses the phosphatase complexes that dephosphorylate eIF-2α. [1]

In vitro: This agent is reported to protect cells from endoplasmic reticulum (ER) stress-induced apoptosis (EC50 ~15 M) in PC12 cell lines induced with the protein glycosylation inhibitor tunicamycin and brefeldin A, which causes ER stress by blocking ER-to-Golgi vesicle transport. Salubrinal is a potentially useful agent to study mechanisms of ER stress-induced apoptosis. In addition, it was reported that salubrinal at 50 μM prevented cells from the autophagic and apoptotic progresses induced by loss of Bcl-2 function in murine leukemia L1210 cells. [1]

In vivo: Study from male ICR mice showed that salubrinal significantly aggravated the cisplatin-induced nephrotoxicity. In the kidneys of cisplatin-treated mice, the phosphorylation of eIF2α was significantly increased by salubrinal. In addition, the expression of CCAAT/enhancer binding protein, activating transcription factor 4 as well as the cleavage of caspases 3, 9 and 12 were also up-regulated. Moreover, salubrinal also increased the cisplatin-induced oxidative stress. These findings indicated that salubrinal aggravated cisplatin-induced nephrotoxicity via the up-regulation of ER stress-related cell apoptosis and oxidative stress. [2]

Clinical trial: So far, no clinical trial has been conducted.

References:
[1] Kessel D.  Protection of Bcl-2 by salubrinal. Biochem Bioph Res Co. 2006; 346: 1320-3.
[2] Wu CT, Sheu ML, Tsai KS, Chiang CK and Liu SH.  Salubrinal, an eIF2α dephosphorylation inhibitor, enhances cisplatin-induced oxidative stress and nephrotoxicity in a mouse model. Free Radic Biol Med, 2011; 51(3): 671-680.

文献引用

Physical AppearanceA solid
StorageStore at -20°C
M.Wt479.81
Cas No.405060-95-9
FormulaC21H17Cl3N4OS
Solubility≥48mg/mL in DMSO
Chemical Name(E)-3-phenyl-N-[2,2,2-trichloro-1-(quinolin-8-ylcarbamothioylamino)ethyl]prop-2-enamide
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)C=CC(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC2=CC=CC3=C2N=CC=C3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。
细胞实验 [1]:

细胞系

PC12细胞

溶解方法

该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

0.5-100 μM处理36小时

应用

Salubrinal抑制由单纯疱疹病毒蛋白介导的eIF2α去磷酸化并阻断病毒复制。Salubrinal剂量依赖性地保护PC12细胞免受内质网(ER)应激诱导的细胞凋亡。 此外,Salubrinal诱导eIF2α磷酸化和选择性抑制eIF2α去磷酸化。

动物实验:

动物模型

大鼠模型

剂量

100μM,1-12小时;静脉注射给药方式

应用

相比对照组,Salubrinal增加深的慢波睡眠和减少主动醒来。 Salubrinal增加p-eIF2α在基底前脑(BF)区(睡眠 - 觉醒调节性脑区)中的表达 [2]。 此外,Salubrinal通过激活睡眠促进神经元和抑制基底前脑(BF)和下丘脑中的唤醒神经元,从而诱导睡眠 [3]。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1Boyce, M., Bryant, K. F., Jousse, C., Long, K., Harding, H. P., Scheuner, D., Kaufman, R. J., Ma, D., Coen, D. M., Ron, D. and Yuan, J. (2005) A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress. Science. 307, 935-939

2Methippara, M. M., Bashir, T., Kumar, S., Alam, N., Szymusiak, R. and McGinty, D. (2009) Salubrinal, an inhibitor of protein synthesis, promotes deep slow wave sleep. Am J Physiol Regul Integr Comp Physiol. 296, R178-184

3Methippara, M., Mitrani, B., Schrader, F. X., Szymusiak, R. and McGinty, D. (2012) Salubrinal, an endoplasmic reticulum stress blocker, modulates sleep homeostasis and activation of sleep- and wake-regulatory neurons. Neuroscience. 209, 108-118

化学结构

Salubrinal

相关生物数据

Salubrinal

相关生物数据

Salubrinal