Salubrinal |
| Catalog No.GC17331 |
Salubrinal is a potent and selective inhibitor of eukaryotic translation initiation factor 2α (eIF2α) dephosphorylation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 405060-95-9
Sample solution is provided at 25 µL, 10mM.
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Salubrinal is a potent and selective inhibitor of eukaryotic translation initiation factor 2α (eIF2α) dephosphorylation[1]. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor, inhibiting anti-collagen antibody-induced arthritis[2]. Salubrinal has anti-HSV-1 viral activity and inhibits the dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5[3].
In vitro, treatment of human skin fibroblasts with Salubrinal (0-20μM) for 1h protected cells from UVB radiation-induced cell death in a dose-dependent manner and maintained intracellular Ca2+ homeostasis[4]. Treatment of bone marrow-derived cells isolated from mice with Salubrinal (1, 2, 5μM) for 6 days inhibited osteoclast differentiation and inhibited migration and adhesion of preosteoclasts in a dose- and time-dependent manner[5].
In vivo, Salubrinal (1mg/kg/day) was treated intraperitoneally in mice with traumatic brain injury (TBI) for 20 days, which effectively reduced TBI-induced plasma membrane permeability, reduced lesion volume, improved neurological deficits, and reduced ER stress-induced autophagy activation[6]. Salubrinal (1mg/kg) was treated intraperitoneally in rats with acute myocardial infarction (MI) for 30min, which increased myocardial eIF2α phosphorylation, reduced the expression of caspase-12 and C/EBP homologous protein (CHOP), and reduced myocardial cell apoptosis and infarct size[7].
References:
[1] Wang R, Sun D Z, Song C Q, et al. Eukaryotic translation initiation factor 2 subunit α (eIF2α) inhibitor salubrinal attenuates paraquat-induced human lung epithelial-like A549 cell apoptosis by regulating the PERK-eIF2α signaling pathway[J]. Toxicology In Vitro, 2018, 46: 58-65.
[2] Hamamura K, Nishimura A, Chen A, et al. Salubrinal acts as a Dusp2 inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis[J]. Cellular signalling, 2015, 27(4): 828-835.
[3] Bryant K F, Macari E R, Malik N, et al. ICP34. 5-dependent and-independent activities of salubrinal in herpes simplex virus-1 infected cells[J]. Virology, 2008, 379(2): 197-204.
[4] Ji C, Yang B, Huang S, et al. Salubrinal protects human skin fibroblasts against UVB-induced cell death by blocking endoplasmic reticulum (ER) stress and regulating calcium homeostasis[J]. Biochemical and biophysical research communications, 2017, 493(4): 1371-1376.
[5] Yokota H, Hamamura K, Chen A, et al. Effects of salubrinal on development of osteoclasts and osteoblasts from bone marrow-derived cells[J]. BMC musculoskeletal disorders, 2013, 14: 1-11.
[6] Wang Z, Gao C, Chen W, et al. Salubrinal offers neuroprotection through suppressing endoplasmic reticulum stress, autophagy and apoptosis in a mouse traumatic brain injury model[J]. Neurobiology of learning and memory, 2019, 161: 12-25.
[7] Li R J, He K L, Li X, et al. Salubrinal protects cardiomyocytes against apoptosis in a rat myocardial infarction model via suppressing the dephosphorylation of eukaryotic translation initiation factor 2α[J]. Molecular Medicine Reports, 2015, 12(1): 1043-1049.
| Cell experiment [1]: | |
Cell lines | Human skin fibroblasts |
Preparation Method | Human skin fibroblasts were pretreated with 0-20μM Salubrinal for 1h and then irradiated with UVB (15mJ/cm2). Cell viability was determined by MTT. |
Reaction Conditions | 0-20μM; 1h |
Applications | Salubrinal protects human skin fibroblasts against UVB radiation-induced cell death in a dose dependent manner. |
| Animal experiment [2]: | |
Animal models | Adult male ICR mice |
Preparation Method | Mice were subjected to Traumatic brain injury (TBI) in the left part of the brain using a weightdrop controlled cortical impact device. After injury, the scalp was sutured and mice returned to their cages to recover from anesthesia. After TBI, mice were sacrificed 6 h, 1 d, 2 d, 3 d, 7 d, 10 d and 14 d after surgery, and control mice were sacrificed on day 2. The groups of this experiment were as follows: vehicle-treated sham group (Sha+Veh), Salubrinal-treated sham group (Sha+Sal), vehicletreated TBI group (TBI+Veh) and Salubrinal-treated TBI group (TBI+Sal). Salubrinal (1mg/kg, first solubilized in DMSO to 100mg/kg and then in saline to the final concentration) was administered by intraperitoneal injection 2h after the onset of TBI and subsequent daily dose for 2 or 21d after TBI. Solvent control mice received a vehicle injection (1% DMSO in saline) at the same time points after TBI. Sham animals also received vehicle or Salubirnal. |
Dosage form | 1mg/kg/day for 20 days; i.p. |
Applications | Salubrinal ameliorated neurological deficits after TBI. Salubrinal reduced lesion volume after TBI. Salubrinal decreased TBI-induced ER stress-autophagic activation. |
References: [1]Ji C, Yang B, Huang S, et al. Salubrinal protects human skin fibroblasts against UVB-induced cell death by blocking endoplasmic reticulum (ER) stress and regulating calcium homeostasis[J]. Biochemical and biophysical research communications, 2017, 493(4): 1371-1376. [2]Wang Z, Gao C, Chen W, et al. Salubrinal offers neuroprotection through suppressing endoplasmic reticulum stress, autophagy and apoptosis in a mouse traumatic brain injury model[J]. Neurobiology of learning and memory, 2019, 161: 12-25. | |
| Cas No. | 405060-95-9 | SDF | |
| Chemical Name | (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 | ||
| Formula | C21H17Cl3N4OS | M.Wt | 479.81 |
| Solubility | ≥ 48mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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