Home Apoptosis PERK inhibitor ISRIB (trans-isomer) For research use only.

ISRIB (trans-isomer)

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

ISRIB (trans-isomer) Chemical Structure

CAS No. 1597403-47-8

Purity & Quality Control

ISRIB (trans-isomer) Related Products

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
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]
Kinase Assay High-content microscopy-based secondary screen [1]
U2OS cells carrying the ATF4-dGFP-IRES-Cherry reporter are plated in 96 well plates and treated with 100 nM Thapsigargin and 10μM of the cherry-picked compounds for 8 hr. Cells are stained with Hoechst 33,258 and are visualized using an automated microscope. Data acquisition and image analyses are performed with the INCell Developer Toolbox Software, version 1.9. Compounds that block induction of the ATF4-dGFP reporter, do not block the accumulation of mCherry downstream of the IRES, and are deemed non-toxic as determined by cell number measured by counting nuclei, are repurchased for further analyses.
Experimental Result Images Methods Biomarkers Images PMID
Western blot PERK / XBP1s / ATF4 23741617
In Vivo
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]
Animal Research Animal Models Male C57BL/6J mice
Dosages 0.25 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 451.34 Formula
C22H24Cl2N2O4
 
 
CAS No. 1597403-47-8 SDF --
Smiles C1CC(CCC1NC(=O)COC2=CC=C(C=C2)Cl)NC(=O)COC3=CC=C(C=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (11.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy ISRIB|ISRIB ic50|ISRIB price|ISRIB cost|ISRIB solubility dmso|ISRIB purchase|ISRIB manufacturer|ISRIB research buy|ISRIB order|ISRIB mouse|ISRIB chemical structure|ISRIB mw|ISRIB molecular weight|ISRIB datasheet|ISRIB supplier|ISRIB in vitro|ISRIB cell line|ISRIB concentration|ISRIB nmr|ISRIB in vivo|ISRIB clinical trial|ISRIB inhibitor|ISRIB Apoptosis inhibitor