Molecular structure of GSK2656157, CAS Number: 1337532-29-2
GSK2656157 (CAS 1337532-29-2)
See product citations (10)
Alternate Names:
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)-ethanone
Application:
GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK
CAS Number:
1337532-29-2
Purity:
≥95%
Molecular Weight:
416.45
Molecular Formula:
C23H21FN6O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK2656157 is a research chemical that acts as an inhibitor of the protein kinase PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase). As an integral part of the unfolded protein response (UPR), PERK plays a critical role in maintaining cellular homeostasis, especially under conditions of endoplasmic reticulum (ER) stress. GSK2656157 is utilized in studies to understand the role of PERK in various cellular processes, including the regulation of protein synthesis and the determination of cell fate decisions during stress conditions. By inhibiting PERK, researchers can investigate its functions and the consequences of its dysregulation, which has implications for understanding diseases associated with ER stress, such as neurodegeneration and cancer. Additionally, GSK2656157 is employed to explore the potential for targeting the UPR pathway in various research models.
GSK2656157 (CAS 1337532-29-2) References
- Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. | Atkins, C., et al. 2013. Cancer Res. 73: 1993-2002. PMID: 23333938
- GSK2656157, a PERK inhibitor, reduced LPS-induced IL-1β production through inhibiting Caspase 1 activation in macrophage-like J774.1 cells. | Ando, T., et al. 2016. Immunopharmacol Immunotoxicol. 38: 298-302. PMID: 27251848
- When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157. | Rojas-Rivera, D., et al. 2017. Cell Death Differ. 24: 1100-1110. PMID: 28452996
- The effect of metformin treatment on endoplasmic reticulum (ER) stress induced by status epilepticus (SE) via the PERK-eIF2α-CHOP pathway. | Chen, J., et al. 2018. Bosn J Basic Med Sci. 18: 49-54. PMID: 28686850
- Low-intensity extracorporeal shock wave therapy promotes myogenesis through PERK/ATF4 pathway. | Wang, B., et al. 2018. Neurourol Urodyn. 37: 699-707. PMID: 28763567
- Simultaneous targeting PI3K and PERK pathways promotes cell death and improves the clinical prognosis in esophageal squamous carcinoma. | Wang, SQ., et al. 2017. Biochem Biophys Res Commun. 493: 534-541. PMID: 28867195
- Attenuation of PERK enhances glucose-stimulated insulin secretion in islets. | Kim, MJ., et al. 2018. J Endocrinol. 236: 125-136. PMID: 29273589
- Aberrant ER Stress Induced Neuronal-IFNβ Elicits White Matter Injury Due to Microglial Activation and T-Cell Infiltration after TBI. | Sen, T., et al. 2020. J Neurosci. 40: 424-446. PMID: 31694961
- Elucidation of the mechanism of NEFA-induced PERK-eIF2α signaling pathway regulation of lipid metabolism in bovine hepatocytes. | Huang, Y., et al. 2021. J Steroid Biochem Mol Biol. 211: 105893. PMID: 33819629
- The effect and apoptosis mechanism of 6-methoxyflavone in HeLa cells. | Zhang, C., et al. 2022. Biomarkers. 27: 470-482. PMID: 35400257
- Molecular modeling provides a structural basis for PERK inhibitor selectivity towards RIPK1. | Chintha, C., et al. 2019. RSC Adv. 10: 367-375. PMID: 35558862
- Toxoplasma gondii dense granule protein 3 promotes endoplasmic reticulum stress-induced apoptosis by activating the PERK pathway. | Obed, C., et al. 2022. Parasit Vectors. 15: 276. PMID: 35918751
- Atractylenolide III Attenuates Apoptosis in H9c2 Cells by Inhibiting Endoplasmic Reticulum Stress through the GRP78/PERK/CHOP Signaling Pathway. | Zuo, MY., et al. 2022. Evid Based Complement Alternat Med. 2022: 1149231. PMID: 36159560
- Depletion and Reversal of Hepatocellular Carcinoma Inducing CTL through ER Stress-Dependent PERK-CHOP Signaling Pathway. | Guo, M., et al. 2022. Can J Gastroenterol Hepatol. 2022: 6413783. PMID: 36262827
- Acute Pharmacological Inhibition of Protein Kinase R-Like Endoplasmic Reticulum Kinase Signaling after Spinal Cord Injury Spares Oligodendrocytes and Improves Locomotor Recovery. | Saraswat Ohri, S., et al. 2023. J Neurotrauma.. PMID: 36503284
Inhibitor of:
nephrin, and PERK.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK2656157, 10 mg | sc-490341 | 10 mg | $165.00 | |||
GSK2656157, 50 mg | sc-490341A | 50 mg | $665.00 | |||
GSK2656157, 100 mg | sc-490341B | 100 mg | $1265.00 | |||
GSK2656157, 250 mg | sc-490341C | 250 mg | $2350.00 |