Salubrinal

Catalog No.S2923

Salubrinal Chemical Structure

Molecular Weight(MW): 479.81

Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.

Size Price Stock Quantity  
In DMSO USD 280 In stock
USD 147 In stock

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  • J Am Soc Nephrol, 2015, 26(8):1839-54. . Salubrinal purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
Targets
eIF2α [1]
(Cell-free assay)
In vitro

Salubrinal is a selective inhibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Salubrinal inhibited ER stress-mediated apoptosis induced by the protein glycosylation inhibitor tunicamycin (Tm) in a dose-dependent manner, with a median effective concentration (EC50) ∼ 15 μM. Salubrinal also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, Salubrinal is not a general apoptosis inhibitor. Salubrinal induced rapid and robust eIF2α phosphorylation and its downstream effects in PC12 cells, including down-regulation of cyclin D1 and up-regulation of GADD34 and CHOP, two proteins whose expression is induced by eIF2α phosphorylation. Salubrinal inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. Salubrinal inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation. [1] Salubrinal increased non-rapid eye movement (NREM) sleep. [2]

In vivo Salubrinal inhibits HSV replication in a mouse cornea infection model. Compared to vehicle control, topical Salubrinal treatment significantly reduced the viral titer recovered from eye swabs of infected animals. [1] I.C.V. administration of Salubrinal significantly modified the homeostatic sleep response. [3]

Protocol

Cell Research
+ Expand
  • Cell lines: PC12
  • Concentrations: 0-100 μM
  • Incubation Time: 48 hours
  • Method: PC12 cells are plated in 384-well plates at 5000 cells per well in 40μL phenol red-freemedium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/mlin DMSO) or National Cancer Institute’s (NCI) Structural Diversity set and Open Collections (10 mM in DMSO) (NCI) are added to the wells by robotic pin transfer. After 48 hours, cell viability is assessed using a luminescence-based ATP assay. DMSO- and zVAD.fmk-treated wells on each plate served as negative and positive controls for rescue from ER stress-induced ATP loss, respectively.
    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: Eight-week-old male CD-1 outbred mice
  • Formulation: in DMEM
  • Dosages: 75μM
  • Administration: On cornea
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (200.07 mM)
Ethanol 2 mg/mL (4.16 mM)
Water <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 479.81
Formula

C21H17Cl3N4OS

CAS No. 405060-95-9
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID