GSK 2606414
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
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.
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Additional Information
Background References
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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:
6 Citations: Showing 1 - 6
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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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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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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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