GSK 2606414

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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)
Citations (16)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

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

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

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

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

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

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