Home ER stress & UPR PERK modulator - phosphatase inhibitor - eIF inhibitor Sal003

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Sal003 PERK modulator

Cat.No.S7437

Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
Sal003 PERK modulator Chemical Structure

Chemical Structure

Molecular Weight: 463.21

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Chemical Information, Storage & Stability

Molecular Weight 463.21 Formula

C18H15Cl4N3OS

 Storage (From the date of receipt)
CAS No. 1164470-53-4 -- Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)C=CC(=O)NC(C(Cl)(Cl)Cl)NC(=S)NC2=CC=C(C=C2)Cl

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (200.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
eIF-2α phosphatase [1]
In vitro
Sal003 increases eIF2α phosphorylation status by blocking eIF2a phosphatases in cells. [1] In mouse embryonic fibroblasts (MEFs), this compound causes dissociation of polysomes by increasing eIF2a phosphorylation. It impairs late-long-term potentiation (L-LTP) in an ATF4-dependent mode in hippocampal slices from WT mice. [2] In addition, eIF2α phosphorylation by this chemical also enhances apoptotic signaling induced by subtilase cytotoxin (SubAB). [3]
In vivo
Sal003 impairs spatial long-term memory formation in rats. [2]
References

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