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Salubrinal Sale

目录号 : GC17331

An inhibitor of eIF dephosphorylation

Salubrinal Chemical Structure

Cas No.:405060-95-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥504.00
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1mg
¥207.00
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5mg
¥455.00
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10mg
¥700.00
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25mg
¥1,400.00
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50mg
¥2,450.00
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100mg
¥4,200.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

PC12 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5-100 μM for 36 hours

Applications

Salubrinal inhibited eIF2a dephosphorylation mediated by a herpes simplex virus protein and blocked viral replication. Salubrinal dose-dependently protected PC12 cells against endoplasmic reticulum (ER) stress-induced apoptosis. Moreover, Salubrinal induced eIF2α phosphorylation and selectively inhibited eIF2α dephosphorylation.

Animal experiment:

Animal models

Rat model;

Dosage form

100 μM for 1-12 hours; i.c.v. administration

Applications

Salubrinal increased deep slow wave sleep and reduced active waking compared with the vehicle. Salubrinal increased expression of p-eIF2α in the basal forebrain (BF) area, a sleep-wake regulatory brain region [2]. Moreover, Salubrinal induced sleep by activating sleep-promoting neurons and inhibiting wake-promoting neurons in the basal forebrain (BF) and hypothalamus [3].

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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

产品描述

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.

Chemical Properties

Cas No. 405060-95-9 SDF
化学名 (E)-3-phenyl-N-[2,2,2-trichloro-1-(quinolin-8-ylcarbamothioylamino)ethyl]prop-2-enamide
Canonical SMILES C1=CC=C(C=C1)C=CC(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC2=CC=CC3=C2N=CC=C3
分子式 C21H17Cl3N4OS 分子量 479.81
溶解度 ≥ 48mg/mL in DMSO 储存条件 4°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0842 mL 10.4208 mL 20.8416 mL
5 mM 0.4168 mL 2.0842 mL 4.1683 mL
10 mM 0.2084 mL 1.0421 mL 2.0842 mL
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