GSK 2606414
1 Image
Description: Potent and selective PERK inhibitor; orally bioavailable
Chemical Name: 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone
Purity: ≥99%
Biological Activity
GSK 2606414 is a potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable.Technical Data
M.Wt:
451.44
Formula:
C24H20F3N5O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
1337531-36-8
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Licensing Caveats:
Sold for research purposes only under agreement from GlaxoSmithKline
Background References
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Casitas B-cell lymphoma (Cbl) proteins protect mammary epithelial cells from proteotoxicity of active c-Src accumulation
Proc. Natl. Acad. Sci. U.S.A, 2016;0(0):. -
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Axten et al.
J.Med.Chem., 2012;55:7193 -
Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK.
Harding et al.
J.Biol.Chem., 2012;287:44338
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Citations for GSK 2606414
The citations listed below are publications that use Tocris products. Selected citations for GSK 2606414 include:
16 Citations: Showing 1 - 10
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Aorta- and liver-generated TMAO enhances trained immunity for increased inflammation via ER stress/mitochondrial ROS/glycolysis pathways.
Authors: Yan Et al.
JCI Insight 2023;8
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ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions
Authors: Jeong Et al.
Exp Mol Med 2023;
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Polyadenylated RNA and RNA-Binding Proteins Exhibit Unique Response to Hyperosmotic Stress.
Authors: Jeffrey D Et al.
Front Cell Dev Biol 2022;9:809859
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Saponin-based adjuvant-induced dendritic cell cross-presentation is dependent on PERK activation.
Authors: Lisa G M Et al.
Cell Mol Life Sci 2022;79:231
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The Unfolded Protein Response Sensor PERK Mediates Stiffness-Dependent Adaptation in Glioblastoma Cells.
Authors: Yuanke Et al.
Int J Mol Sci 2022;23
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LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells.
Authors: Chong-Shan Et al.
Autophagy 2022;18:204-222
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PERK signaling through C/EBPδ contributes to ER stress-induced expression of immunomodulatory and tumor promoting chemokines by cancer cells.
Authors: Vishal N Et al.
Cell Death Dis 2021;12:1038
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The integrated stress response promotes B7H6 expression.
Authors: Ofer Et al.
J Mol Med (Berl) 2020;98:135-148
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Aripiprazole Cytotoxicity Coincides with Activation of the Unfolded Protein Response in Human Hepatic Cells.
Authors: Angela M Et al.
J Pharmacol Exp Ther 2020;374:452-461
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Pharmacological induction of selective endoplasmic reticulum retention as a strategy for cancer therapy.
Authors: Christian Et al.
Nat Commun 2020;11:1304
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Cytosolic translational responses differ under conditions of severe short-term and long-term mitochondrial stress.
Authors: Samluk Et al.
Mol Biol Cell 2019;:mbcE18100628
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Probing the Global Cellular Responses to Lipotoxicity Caused by Saturated Fatty Acids.
Authors: J Wade Et al.
Mol Cell 2019;74:32-44.e8
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The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors.
Authors: Mahameed Et al.
Cell Death Dis 2019;10:300
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Quantitative proteomics identifies redox switches for global translation modulation by mitochondrially produced reactive oxygen species.
Authors: Topf Et al.
Nat Commun 2018;9:324
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Modulation of Protein Synthesis by eIF2α Phosphorylation Protects Cell from Heat Stress-Mediated Apoptosis.
Authors: Park Et al.
Cells 2018;7
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Expansion of DUB functionality generated by alternative isoforms - USP35, a case study.
Authors: Leznicki Et al.
J Cell Sci 2018;131
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