Salubrinal

Catalog No.S2923 Batch:S292301

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Technical Data

Formula

C21H17Cl3N4OS
Molecular Weight 479.81 CAS No. 405060-95-9
Solubility (25°C)* In vitro DMSO 96 mg/mL (200.07 mM)
Ethanol 2 mg/mL (4.16 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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). This compound 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. It also suppressed Tm-induced DNA fragmentation the processing of caspase-7, a caspase activated by ER stress. However, this chemical is not a general apoptosis inhibitor. It 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. This inhibitor inhibits eIF2α dephosphorylation by inhibiting the PP1/GADD34 complex. It inhibits HSV replication with IC50 of ~ 3μM by inhibiting eIF2α dephosphorylation. [1] This compound 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 treatment with this compound significantly reduced the viral titer recovered from eye swabs of infected animals. [1] I.C.V. administration of this chemical significantly modified the homeostatic sleep response. [3]

Protocol (from reference)

Cell Assay:

[1]
  • 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-free medium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/ml in 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.
Animal Study:

[1]
  • Animal Models

    Eight-week-old male CD-1 outbred mice

  • Dosages

    75μM

  • Administration

    On cornea

References

  • https://pubmed.ncbi.nlm.nih.gov/15705855/
  • http://www.ncbi.nlm.nih.gov/pubmed?term=18971348
  • http://www.ncbi.nlm.nih.gov/pubmed?term=22387272

Customer Product Validation

<p>AngII (30 minutes)-induced Akt activation was attenuated by the ER stress inhibitors 4-PBA (5 mM, 2 hours), TUDCA (300 µg/ml, 1 hour), and salubrinal (30 µM, 1 hour) (n=5; *P<0.01 versus con, #P<0.05 versus Ang)</p>

, , J Am Soc Nephrol, 2015, 26(8):1839-54.

PC-3 and HCT-116 p53+/+ cells were treated with 3-AWA and/or salubrinal for the indicated time point. The protein-specific antibodies were used to analyze the expression of the given proteins through immunoblotting.

Data from [ , , Oncogenesis, 2017, 6(5):e341 ]

HEK293 cells were transfected with or without Flag-VP1 for 24 h, then treated with d Salubrinal (Sal, 75 μM) for 8 h followed by immunoblot detection. All data in this figure represent the mean ± SEM of three independent experiments. *p<0.05; ***p<0.01.

Data from [ , , Neurotox Res, 2017, 31(2):204-217 ]

Selleck's Salubrinal Has Been Cited by 44 Publications

Suppressing protein damage response to overcome multidrug resistance in cancer therapy [ Cell Discov, 2025, 11(1):80] PubMed: 41027888
The integrated stress response fine-tunes stem cell fate decisions upon serine deprivation and tissue injury [ Cell Metab, 2025, 37(8):1715-1731.e11] PubMed: 40513561
The integrated stress response drives MET oncogene overexpression in cancers [ EMBO J, 2025, 44(4):1107-1130] PubMed: 39774381
Repressing cytokine storm-like response in macrophages by targeting the eIF2α-integrated stress response pathway [ Int Immunopharmacol, 2025, 147:113965] PubMed: 39752757
CB-5083 and luteolin synergistically induce the apoptosis of bladder cancer cells via multiple mechanisms [ Toxicol Appl Pharmacol, 2025, 499:117333] PubMed: 40194745
Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31] PubMed: 38212315
GDF15 ameliorates sepsis-induced lung injury via AMPK-mediated inhibition of glycolysis in alveolar macrophage [ Respir Res, 2024, 25(1):201] PubMed: 38725041
Multiplex single-cell chemical genomics reveals the kinase dependence of the response to targeted therapy [ Cell Genom, 2024, 4(2):100487] PubMed: 38278156
Neurotransmitter release progressively desynchronizes in induced human neurons during synapse maturation and aging [ Cell Rep, 2023, 42(2):112042] PubMed: 36701235
Lovastatin Treatment Inducing Apoptosis in Human Pancreatic Cancer Cells by Inhibiting Cholesterol Rafts in Plasma Membrane and Mitochondria [ Int J Mol Sci, 2023, 24(23)16814] PubMed: 38069135

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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