Salubrinal

Catalog No.S2923 Batch:S292304

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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 3 mg/mL (6.25 mM)
Water Insoluble
* <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.)

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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 (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-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.
Animal Study:

[1]
  • Animal Models

    Eight-week-old male CD-1 outbred mice

  • Dosages

    75μM

  • Administration

    On cornea

Customer Product Validation

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

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

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

Selleck's Salubrinal has been cited by 38 publications

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
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
Nuclear fragile X mental retardation-interacting protein 1-mediated ribophagy protects T lymphocytes against apoptosis in sepsis [ Burns Trauma, 2023, 11:tkac055] PubMed: 36873287
Hesperadin suppresses pancreatic cancer through ATF4/GADD45A axis at nanomolar concentrations [ Oncogene, 2022, 10.1038/s41388-022-02328-4] PubMed: 35551503
PARP1 Might Substitute HSF1 to Reactivate Latent HIV-1 by Binding to Heat Shock Element [ Cells, 2022, 11(15)2331] PubMed: 35954175
Neurodegeneration Risk Factor, EIF2AK3 (PERK), Influences Tau Protein Aggregation [ J Biol Chem, 2022, S0021-9258(22)01264-9] PubMed: 36563857
Pazopanib restricts small cell lung cancer proliferation via reactive oxygen species-mediated endoplasmic reticulum stress [ Thorac Cancer, 2022, 13(17):2421-2428] PubMed: 35866204
mTORC1 couples cyst(e)ine availability with GPX4 protein synthesis and ferroptosis regulation [ Nat Commun, 2021, 12(1):1589] PubMed: 33707434

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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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