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Submit ReviewGSK 2606414
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% (HPLC)
Biological Activity for GSK 2606414
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.
Licensing Information
Sold for research purposes only under agreement from GlaxoSmithKline
Compound Libraries for GSK 2606414
GSK 2606414 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK 2606414
| M. Wt | 451.44 |
| Formula | C24H20F3N5O |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1337531-36-8 |
| PubChem ID | 53469448 |
| InChI Key | SIXVRXARNAVBTC-UHFFFAOYSA-N |
| Smiles | NC1=NC=NC2=C1C(C3=CC(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4C=C3)=CN2C |
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.
Solubility Data for GSK 2606414
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.14 | 100 |
Preparing Stock Solutions for GSK 2606414
The following data is based on the product molecular weight 451.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.22 mL | 11.08 mL | 22.15 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.43 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for GSK 2606414
References for GSK 2606414
References are publications that support the biological activity of the product.
Axten et al (2012) 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). J.Med.Chem. 55 7193 PMID: 22827572
Harding et al (2012) Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 287 44338 PMID: 23148209
If you know of a relevant reference for GSK 2606414, please let us know.
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Keywords: GSK 2606414, GSK 2606414 supplier, GSK2606414, potent, selective, protein, kinase, R-like, ER, PERK, orally, bioavailable, antitumor, ER-stress, 5107, Tocris Bioscience
16 Citations for GSK 2606414
Citations are publications that use Tocris products. Selected citations for GSK 2606414 include:
Park et al (2018) Modulation of Protein Synthesis by eIF2α Phosphorylation Protects Cell from Heat Stress-Mediated Apoptosis. Cells 7 PMID: 30544621
Vishal N et al (2021) PERK signaling through C/EBPδ contributes to ER stress-induced expression of immunomodulatory and tumor promoting chemokines by cancer cells. Cell Death Dis 12 1038 PMID: 34725321
Samluk et al (2019) Cytosolic translational responses differ under conditions of severe short-term and long-term mitochondrial stress. Mol Biol Cell mbcE18100628 PMID: 31116686
Yuanke et al (2022) The Unfolded Protein Response Sensor PERK Mediates Stiffness-Dependent Adaptation in Glioblastoma Cells. Int J Mol Sci 23 PMID: 35742966
Chong-Shan et al (2022) LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells. Autophagy 18 204-222 PMID: 34313548
Jeffrey D et al (2022) Polyadenylated RNA and RNA-Binding Proteins Exhibit Unique Response to Hyperosmotic Stress. Front Cell Dev Biol 9 809859 PMID: 34970554
Lisa G M et al (2022) Saponin-based adjuvant-induced dendritic cell cross-presentation is dependent on PERK activation. Cell Mol Life Sci 79 231 PMID: 35396971
Mahameed et al (2019) The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis 10 300 PMID: 30931942
Leznicki et al (2018) Expansion of DUB functionality generated by alternative isoforms - USP35, a case study. J Cell Sci 131 PMID: 29685892
J Wade et al (2019) Probing the Global Cellular Responses to Lipotoxicity Caused by Saturated Fatty Acids. Mol Cell 74 32-44.e8 PMID: 30846318
Topf et al (2018) Quantitative proteomics identifies redox switches for global translation modulation by mitochondrially produced reactive oxygen species. Nat Commun 9 324 PMID: 29358734
Angela M et al (2020) Aripiprazole Cytotoxicity Coincides with Activation of the Unfolded Protein Response in Human Hepatic Cells. J Pharmacol Exp Ther 374 452-461 PMID: 32554435
Ofer et al (2020) The integrated stress response promotes B7H6 expression. J Mol Med (Berl) 98 135-148 PMID: 31838577
Christian et al (2020) Pharmacological induction of selective endoplasmic reticulum retention as a strategy for cancer therapy. Nat Commun 11 1304 PMID: 32161259
Yan et al (2023) Aorta- and liver-generated TMAO enhances trained immunity for increased inflammation via ER stress/mitochondrial ROS/glycolysis pathways. JCI Insight 8 PMID: 36394956
Jeong et al (2023) ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions Exp Mol Med PMID: 36759578
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Cell Cycle and DNA Damage Research Product Guide
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