Name: Salubrinal
Price: 349.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
    
    [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.
- Properties
  - Alternative Name
    
    (E)-3-phenyl-N-[2,2,2-trichloro-1-(quinolin-8-ylcarbamothioylamino)ethyl]prop-2-enamide
    
    CAS Number
    
    405060-95-9
    
    Molecular Formula
    
    C21H17Cl3N4OS
    
    Molecular Weight
    
    479.81
    
    Appearance
    
    A solid
    
    Purity
    
    99.64%
    
    Solubility
    
    ≥48 mg/mL in DMSO; insoluble in H2O; ≥2.2 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Rochelle Fletcher, Jingshan Tong, et al. "Non-steroidal anti-inflammatory drugs induce immunogenic cell death in suppressing colorectal tumorigenesis." Oncogene. 2021 Mar;40(11):2035-2050. PMID:33603166
    2. Yang, Jian-wen, and Zhi-ping Hu. "Neuroprotective effects of atorvastatin against cerebral ischemia/reperfusion injury through the inhibition of endoplasmic reticulum stress." Neural Regeneration Research 10.8 (2015): 1239.

Salubrinal

Salubrinal

Background

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