Salubrinal

For research use only.

Catalog No.S2923

26 publications

Salubrinal Chemical Structure

CAS No. 405060-95-9

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

Selleck's Salubrinal has been cited by 26 publications

Purity & Quality Control

Choose Selective PERK Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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LB2241-RCC NUPwNmdvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDRwOUi1O|Ih|ryPLh?= NFXtbWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkevK|5USU6JRWK8M4E,
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NEC8 NYr4ZppGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrBTY5pcWKrdHnvckBw\iCqdX3hckBPTUN6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC2MlA2OzNzIN88UU4> NHnjTJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkevK|5USU6JRWK8M4E,
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MRK-nu-1 M{X2Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmLpTY5pcWKrdHnvckBw\iCqdX3hckBOWktvboWtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPy55NUG3NUDPxE1w M2TUOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE5ODF{Nz:nQnNCVkeHUkyvZV4>
LB2518-MEL MlH0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDdwOUezNlYh|ryPLh?= NVzMRnpiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUK3M{c,W0GQR1XSQE9iRg>?
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ATF4 ; 

PubMed: 27729194     


OVCAR10 cells were incubated with sub-lethal dose of Salubrinal [20 μM] for 1, 3, 6, 12, 24 and 48 h. Whole cell lysates were subjected to Western blot analysis and probed with the above antibodies.

HSF1 / p-HSF1 / ATF3 / c-fos / NFATc1 / RelA ; 

PubMed: 27189267     


The accumulation of cellular transcription factors in nucleus was analyzed after treatment with salubrinal for 4 hours.

GRP78 / p-eIF2α / CHOP ; 

PubMed: 24525736     


HepG2 cells were treated with salubrinal at the indicated dosages for 24 h. Total proteins were harvested and subjected to western blotting analysis of GRP78, P-eIF2α, CHOP and β-actin. 

27729194 27189267 24525736
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:[1]
- Collapse
  • 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:[1]
- Collapse
  • Animal Models: Eight-week-old male CD-1 outbred mice
  • Dosages: 75μM
  • Administration: On cornea
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (197.99 mM)
Water Insoluble
Ethanol '2 mg/mL

* 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
Smiles C1=CC=C(C=C1)C=CC(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC2=CC=CC3=C2N=CC=C3

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID