Salubrinal

Catalog No.S2923 Batch:S292303

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

5 mg/mL (10.42 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.6mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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). 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

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

References

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.