Date published: 2025-10-15

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GSK PERK Inhibitor Inhibitor (CAS 1337531-89-1)

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Alternate Names:
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone
CAS Number:
1337531-89-1
Molecular Weight:
469.43
Molecular Formula:
C24H19F4N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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The GSK PERK inhibitor stands as a remarkable small molecule compound designed to target the protein kinase RNA-like endoplasmic reticulum kinase (PERK). PERK assumes a pivotal role as a regulator within the unfolded protein response (UPR) pathway, which holds paramount importance in maintaining cellular homeostasis. Activation of the UPR pathway occurs in response to endoplasmic reticulum (ER) stress, provoked by the accumulation of misfolded proteins within the ER. Upon activation, the UPR pathway orchestrates the reduction of protein synthesis and the upregulation of genes involved in protein folding and degradation. The proposed mechanism of action revolves around inhibiting GSK PERK-mediated phosphorylation of eIF2α, which subsequently curtails protein synthesis while augmenting the expression of genes involved in protein folding and degradation.


GSK PERK Inhibitor Inhibitor (CAS 1337531-89-1) References

  1. A close connection between the PERK and IRE arms of the UPR and the transcriptional regulation of autophagy.  |  Deegan, S., et al. 2015. Biochem Biophys Res Commun. 456: 305-11. PMID: 25475719
  2. The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.  |  Sidrauski, C., et al. 2015. Elife. 4: PMID: 25719440
  3. Assays for induction of the unfolded protein response and selective activation of the three major pathways.  |  Gupta, A., et al. 2015. Methods Mol Biol. 1292: 19-38. PMID: 25804745
  4. Pharmacological dimerization and activation of the exchange factor eIF2B antagonizes the integrated stress response.  |  Sidrauski, C., et al. 2015. Elife. 4: e07314. PMID: 25875391
  5. Endoplasmic reticulum stress-independent activation of unfolded protein response kinases by a small molecule ATP-mimic.  |  Mendez, AS., et al. 2015. Elife. 4: PMID: 25986605
  6. NCOA3 coactivator is a transcriptional target of XBP1 and regulates PERK-eIF2α-ATF4 signalling in breast cancer.  |  Gupta, A., et al. 2016. Oncogene. 35: 5860-5871. PMID: 27109102
  7. The ER Stress Sensor PERK Coordinates ER-Plasma Membrane Contact Site Formation through Interaction with Filamin-A and F-Actin Remodeling.  |  van Vliet, AR., et al. 2017. Mol Cell. 65: 885-899.e6. PMID: 28238652
  8. Hyperactivation of nuclear receptor coactivators induces PERK-dependent cell death.  |  Hossain, MM., et al. 2018. Oncotarget. 9: 11707-11721. PMID: 29545931
  9. Perturbation of ubiquitin homeostasis promotes macrophage oxidative defenses.  |  Charbonneau, ME., et al. 2019. Sci Rep. 9: 10245. PMID: 31308397
  10. Endoplasmic reticulum as a potential therapeutic target for covid-19 infection management?  |  Sureda, A., et al. 2020. Eur J Pharmacol. 882: 173288. PMID: 32561291
  11. Simvastatin Induces Unfolded Protein Response and Enhances Temozolomide-Induced Cell Death in Glioblastoma Cells.  |  Dastghaib, S., et al. 2020. Cells. 9: PMID: 33105603
  12. Autophagy, Unfolded Protein Response, and Neuropilin-1 Cross-Talk in SARS-CoV-2 Infection: What Can Be Learned from Other Coronaviruses.  |  Siri, M., et al. 2021. Int J Mol Sci. 22: PMID: 34206057

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

GSK PERK Inhibitor, 1 mg

sc-490139
1 mg
$300.00