ISRIB (trans-isomer)
Based on 46 publication(s) in Google Scholar
ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 1597403-47-8
- Formula: C22H24Cl2N2O4
- Molecular Weight:451.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) ISRIB (trans-isomer)
More- Signal Transduct Target Ther. 2025 Dec 17;10(1):413. [Abstract]
- Nature. 2026 Apr;652(8112):1339-1348. [Abstract]
- Cell. 2022 Sep 1;185(18):3356-3374.e22. [Abstract]
- Cell Res. 2026 Jan 28. [Abstract]
- Nat Metab. 2026 Jan;8(1):139-158. [Abstract]
- Cell Stem Cell. 2025 Oct 2;32(10):1509-1527.e9. [Abstract]
- Nat Cell Biol. 2024 Jun;26(6):917-931. [Abstract]
- Adv Funct Mater. 2025 Apr 21.
- Nat Commun. 2022 Nov 10;13(1):6796. [Abstract]
- Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
- Biomaterials. 2021 May:272:120757. [Abstract]
- J Hazard Mater. 2025 Sep 15:496:139407. [Abstract]
- Pharmacol Res. 2022 Aug:182:106285. [Abstract]
- Cell Mol Biol Lett. 2023 Oct 12;28(1):79. [Abstract]
- Cell Mol Biol Lett. 2022 Dec 16;27(1):110. [Abstract]
- Diabetologia. 2021 May;64(5):1144-1157. [Abstract]
- Cell Death Dis. 2024 Jun 19;15(6):431. [Abstract]
- Cell Death Dis. 2023 Jun 14;14(6):361. [Abstract]
- Apoptosis. 2026 Jan 12;31(1):42. [Abstract]
- Biomed Pharmacother. 2023 Jan:157:114037. [Abstract]
- Oncogene. 2017 Nov 30;36(48):6738-6746. [Abstract]
- Cell Death Discov. 2022 Dec 16;8(1):493. [Abstract]
- Elife. 2020 Jun 2;9:e54954. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 15:270:115895. [Abstract]
- Mol Ther Nucleic Acids. 2023 Jul 15:33:286-295. [Abstract]
- J Mater Chem B. 2021 Oct 6;9(38):8109-8120. [Abstract]
- Int J Mol Sci. 2022 Jun 16;23(12):6727. [Abstract]
- Eur J Pharmacol. 2025 Dec 10:1011:178457. [Abstract]
- Cancers (Basel). 2025 Dec 27;18(1):92. [Abstract]
- iScience. 2025 Nov 30.
- Microbiol Spectr. 2022 Dec 21;10(6):e0328222. [Abstract]
- J Virol. 2018 Jul 31;92(16). pii: e00600-18. [Abstract]
- Viruses. 2026 Feb 12;18(2):229. [Abstract]
- Am J Physiol Gastrointest Liver Physiol. 2025 Apr 17. [Abstract]
- J Mol Neurosci. 2022 Mar;72(3):585-597. [Abstract]
- Patent. US20250295610A1.
- bioRxiv. 2025 Aug 31:2025.08.26.672367. [Abstract]
- bioRxiv. 2025 March 19.
- bioRxiv. 2025 February 06.
- bioRxiv. 2024 Nov 03.
- bioRxiv. 2024 July 05.
- bioRxiv. 2024 Jun 3:2023.10.06.561126. [Abstract]
- University of Gothenburg. 2023 Jun 27.
- Research Square Print. September 9th, 2022.
- Research Square Print. 2022 Jun.
- Universidad de Granada. 2020 Sep.
Customer Validation & Images
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RT-PCR
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Cell Imaging/Staining
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RT-PCR
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
Biological Activity
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PERK 5 nM (IC50) |
Trans-ISRIB is 100-fold more potent (IC50=5 nM) than cis-ISRIB (IC50= 600 nM), indicating that the compound’s interaction with its cellular target is stereospecific. ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress[1]. ISRIB substantially reverses the translational effects elicited by phosphorylation of eIF2α and induces no major changes in translation or mRNA levels in unstressed cells. eIF2α phosphorylation-induced stress granule (SG) formation is blocked by ISRIB[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1597403-47-8
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Appearance Solid
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Molecular Weight 451.34
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Formula C22H24Cl2N2O4
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Color White to off-white
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SMILES
O=C(N[C@H]1CC[C@H](NC(COC2=CC=C(Cl)C=C2)=O)CC1)COC3=CC=C(Cl)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (46)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Disruption of heme homeostasis by nuclear receptor Nur77 induces pyroptosis through granzyme B-dependent GSDMC cleavage. [Abstract]2025 Dec 17;10(1):413. PMID: 41407678
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 17;10(1):413. [Abstract]
Cells were cotreated with ISRIB (5 μM) and DdBIC to determine the mRNA levels of GZMB.
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Nature
2026 Apr;652(8112):1339-1348. PMID: 41813904 -
Cell
2022 Sep 1;185(18):3356-3374.e22. PMID: 36055199
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Cell. 2022 Sep 1;185(18):3356-3374.e22. [Abstract]
Double-luciferase assay of WT or BAX, BAK, BOK TKO PC9 cells expressing ATF4 translation reporter and treated with ISRIB 100 μM overnight.
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Cell Res
2026 Jan 28. PMID: 41606169 -
Nat Metab
Single-cell perturbations decipher ribosomal stress-surveillance regulators in type 2 diabetes. [Abstract]2026 Jan;8(1):139-158. PMID: 41482566 -
Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Nat Cell Biol
2024 Jun;26(6):917-931. PMID: 38714852 -
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2025 Apr 21.
ISRIB (200 nM; 8-72h). The fluorescence intensity of GFP protein in BMDCs, DC2.4, and RAW264.7 were analyzed. Student's t-test, compared to mRNA only group.
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Nat Commun
Maprotiline restores ER homeostasis and rescues neurodegeneration via Histamine Receptor H1 inhibition in retinal ganglion cells. [Abstract]2022 Nov 10;13(1):6796. PMID: 36357388 -
Adv Sci (Weinh)
PERK-Mediated Cholesterol Excretion from IDH Mutant Glioma Determines Anti-Tumoral Polarization of Microglia. [Abstract]2023 Jul;10(20):e2205949. PMID: 37166058
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
RT-qPCR analysis of miR‐19a expression in IDHmt U87 cells treated with ISRIB (0-20 μM) in a concentration gradient for 24 h. RNU6B is used as an internal control.
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
ISRIB (10 μM; 48 h). Representative images of BODIPY staining in BV2 cells cultured for 48 h in five types of medium.
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Biomaterials
Targeted regulation of lymphocytic ER stress response with an overall immunosuppression to alleviate allograft rejection. [Abstract]2021 May:272:120757. PMID: 33798960 -
J Hazard Mater
Excessive mitochondrial stress response triggers neuronal injury through the persistent eIF2α phosphorylation in mice exposed to manganese. [Abstract]2025 Sep 15:496:139407. PMID: 40763529 -
Pharmacol Res
Diterpenoid Vinigrol specifically activates ATF4/DDIT3-mediated PERK arm of unfolded protein response to drive non-apoptotic death of breast cancer cells. [Abstract]2022 Aug:182:106285. PMID: 35662627 -
Cell Mol Biol Lett
Activation of BZW1 by CEBPB in macrophages promotes eIF2α phosphorylation-mediated metabolic reprogramming and endoplasmic reticulum stress in MRL/lpr lupus-prone mice. [Abstract]2023 Oct 12;28(1):79. PMID: 37828427 -
Cell Mol Biol Lett
Metabolic disorders sensitise endometrial carcinoma through endoplasmic reticulum stress. [Abstract]2022 Dec 16;27(1):110. PMID: 36526973 -
Diabetologia
Saturated fatty acids entrap PDX1 in stress granules and impede islet beta cell function. [Abstract]2021 May;64(5):1144-1157. PMID: 33569632 -
Cell Death Dis
Syrosingopine and UK5099 synergistically suppress non-small cell lung cancer by activating the integrated stress response. [Abstract]2024 Jun 19;15(6):431. PMID: 38898028 -
Cell Death Dis
SMURF1 attenuates endoplasmic reticulum stress by promoting the degradation of KEAP1 to activate NRF2 antioxidant pathway. [Abstract]2023 Jun 14;14(6):361. PMID: 37316499 -
Apoptosis
Propofol attenuates angiogenesis by activating endoplasmic reticulum stress to suppress TFAP2C-driven VEGFA transcription. [Abstract]2026 Jan 12;31(1):42. PMID: 41524974 -
Biomed Pharmacother
Remdesivir inhibits the progression of glioblastoma by enhancing endoplasmic reticulum stress. [Abstract]2023 Jan:157:114037. PMID: 36427388 -
Oncogene
Knockdown of IRE1α inhibits colonic tumorigenesis through decreasing β-catenin and IRE1α targeting suppresses colon cancer cells. [Abstract]2017 Nov 30;36(48):6738-6746. PMID: 28825721
ISRIB (trans-isomer) purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 Nov 30;36(48):6738-6746. [Abstract]
ISRIB reverses the expression of β-catenin. HCT116 cells are transfected and CT26.WT cells are infected for 48 and 72 h, respectively. The cells are treated with ISRIB (100 nM) for 24 h.
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Cell Death Discov
Cysteine dioxygenase 1 attenuates the proliferation via inducing oxidative stress and integrated stress response in gastric cancer cells. [Abstract]2022 Dec 16;8(1):493. PMID: 36526626 -
Elife
MARCH5 mediates NOXA-dependent MCL1 degradation driven by kinase inhibitors and integrated stress response activation. [Abstract]2020 Jun 2;9:e54954. PMID: 32484436 -
Ecotoxicol Environ Saf
The impact of tetrachlorobisphenol A exposure during puberty: Altered Leydig cell development and induced endoplasmic reticulum stress in male mice. [Abstract]2024 Jan 15:270:115895. PMID: 38159341 -
Mol Ther Nucleic Acids
RGC-specific ATF4 and/or CHOP deletion rescues glaucomatous neurodegeneration and visual function. [Abstract]2023 Jul 15:33:286-295. PMID: 37547290 -
J Mater Chem B
Dual-responsive ultrathin 1T-phase niobium telluride nanosheet-based delivery systems for enhanced chemo-photothermal therapy. [Abstract]2021 Oct 6;9(38):8109-8120. PMID: 34494067 -
Int J Mol Sci
Lysine Deprivation Regulates Npy Expression via GCN2 Signaling Pathway in Mandarin Fish (Siniperca chuatsi). [Abstract]2022 Jun 16;23(12):6727. PMID: 35743178 -
Eur J Pharmacol
Targeting the integrated stress response with ISRIB enhances CREB/BDNF signaling and attenuates cognitive deficits in a rat model of vascular cognitive impairment. [Abstract]2025 Dec 10:1011:178457. PMID: 41380823 -
Cancers (Basel)
Synthesis and Biological Evaluation of a Caffeic Acid Phenethyl Ester Derivatives as Anti-Hepatocellular Carcinoma Agents via Inhibition of Mitochondrial Respiration and Disruption of Cellular Metabolism. [Abstract]2025 Dec 27;18(1):92. PMID: 41514605 -
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Microbiol Spectr
African Swine Fever Virus MGF110-7L Induces Host Cell Translation Suppression and Stress Granule Formation by Activating the PERK/PKR-eIF2α Pathway. [Abstract]2022 Dec 21;10(6):e0328222. PMID: 36377947 -
J Virol
Porcine Reproductive and Respiratory Syndrome Virus Infection Induces both eIF2α Phosphorylation-Dependent and -Independent Host Translation Shutoff. [Abstract]2018 Jul 31;92(16). pii: e00600-18. PMID: 29899101 -
Viruses
ASFV MGF110-7L Inhibits eIF4G1 Expression via Endoplasmic Reticulum Stress to Block Host Translation. [Abstract]2026 Feb 12;18(2):229. PMID: 41754572 -
Am J Physiol Gastrointest Liver Physiol
Saturated phosphatidic acids induce mTORC1-driven integrated stress response contributing to glucolipotoxicity in hepatocytes. [Abstract]2025 Apr 17. PMID: 40241617 -
J Mol Neurosci
Attenuation of Activated eIF2α Signaling by ISRIB Treatment After Spinal Cord Injury Improves Locomotor Function. [Abstract]2022 Mar;72(3):585-597. PMID: 34647267 -
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bioRxiv
Replating induces mTOR-dependent rescue of protein synthesis in Charcot-Marie-Tooth diseased neurons. [Abstract]2025 Aug 31:2025.08.26.672367. PMID: 40909707 -
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bioRxiv
Inhibition of the Eukaryotic Initiation Factor-2-α Kinase PERK Decreases Risk of Autoimmune Diabetes in Mice. [Abstract]2024 Jun 3:2023.10.06.561126. PMID: 38895427 -
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Solvent & Solubility
DMSO : 4.55 mg/mL (10.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 0.83 mg/mL (1.84 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
Protocol
U2OS cells are plated on 96-well plates and left to recover overnight. Cells are treated with either with 2 µg/ml tunicamycin or 100 nM thapsigargin in the presence or absence of 100 nM ISRIB or with ISRIB alone for the indicated and the level of eIF2α phosphorylation is determined[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Intra-peritoneal (ip) route of administration is performed on 6-7 wk old female CD-1 mice. Animals receives a single, 5 mg/kg dose in groups of three mice/compound/route of administration. ISRIB is dissolved in DMSO then diluted 1:1 in Super-Refined PEG 400. Blood (80 μL) is collected from the saphenous vein at intervals post-dosing (20 min, 1 hr, 3 hr, 8 hr, 24 hr) in EDTA containing collection tubes and plasma is prepared for analysis. Compounds are detected by time-of-flight mass spectroscopy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Sidrauski C, et al. Pharmacological brake-release of mRNA translation enhances cognitive memory. Elife. 2013 May 28;2:e00498. [Content Brief]
[2]. Sidrauski C, et al. The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stressgranule assembly. Elife. 2015 Feb 26;4. doi: 10.7554/eLife.05033. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2156 mL | 11.0781 mL | 22.1562 mL | 55.3906 mL |
| 5 mM | 0.4431 mL | 2.2156 mL | 4.4312 mL | 11.0781 mL | |
| 10 mM | 0.2216 mL | 1.1078 mL | 2.2156 mL | 5.5391 mL |
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