ISRIB (trans-isomer)

Catalog No.S7400

For research use only.

ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells.

ISRIB (trans-isomer) Chemical Structure

CAS No. 1597403-47-8

Selleck's ISRIB (trans-isomer) has been cited by 5 Publications

1 Customer Review

Purity & Quality Control

Choose Selective PERK Inhibitors

Biological Activity

Description ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells.
Targets
PERK [1]
(Cell-free assay)
5 nM
In vitro

ISRIB blocks production of endogenous ATF4, whereas XBP1 mRNA splicing and XBP1s production persisted. ISRIB prevents cells from re-establishing ER homeostasis by blocking signaling through the PERK branch of the UPR, and decreases the viability of cells that are subjected to ER-stress. [1]

Assay
Methods Test Index PMID
Western blot PERK / XBP1s / ATF4 23741617
In vivo ISRIB shows favorable properties in pharmacokinetic profiling experiments and good bioavailability in vivo. ISRIB (0.25 mg/kg i.p.) increases long-term memory in mice by enhancing spatial and fear-associated learning. [1]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Male C57BL/6J mice
  • Dosages: 0.25 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 451.34
Formula
C22H24Cl2N2O4
 
 
CAS No. 1597403-47-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1NC(=O)COC2=CC=C(C=C2)Cl)NC(=O)COC3=CC=C(C=C3)Cl

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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.

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Molarity Calculator

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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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