ISRIB (trans-isomer)

For research use only.

Catalog No.S7400

4 publications

ISRIB (trans-isomer) Chemical Structure

Molecular Weight(MW): 451.34

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.

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Selleck's ISRIB (trans-isomer) has been cited by 4 publications

1 Customer Review

  • PERK inhibitor treatment restores female development in zar1 homozygous mutants. Juveniles were treated with two PERK inhibitors from 22 dpf to 60 dpf. Final concentration: ISRIB, 50 nM. **P<0.01, ***P<0.001.

    Development, 2017, 144(1):128-138. ISRIB (trans-isomer) purchased from Selleck.

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 ; 

PubMed: 23741617     


Effect of ISRIB on production of endogenous ATF4, PERK phosphorylation, and XBP1s production. An immunoblot analysis of PERK, ATF4 and XBP1s in HEK293T cells treated with different ER stress inducers (2.5 µg/ml tunicamycin [Tm] or 100 nM thapsigargin [Tg]) with or without 200 nM ISRIB for 3 hr is shown. The arrowhead marks the XBP1s specific band. 

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

Animal Research:

[1]

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  • Animal Models: Male C57BL/6J mice
  • Dosages: 0.25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL (8.86 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 451.34
Formula
C22H24Cl2N2O4
 
 
CAS No. 1597403-47-8
Storage powder
in solvent
Synonyms N/A
Smiles ClC1=CC=C(OCC(=O)NC2CCC(CC2)NC(=O)COC3=CC=C(Cl)C=C3)C=C1

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID