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Submit ReviewGSK 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.
Sold for research purposes only under agreement from GlaxoSmithKline
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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 45.14 | 100 |
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 |
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.
Keywords: GSK 2606414, GSK 2606414 supplier, GSK2606414, potent, selective, protein, kinase, R-like, ER, PERK, orally, bioavailable, antitumor, ER-stress, 5107, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for GSK 2606414 include:
Jeong et al (2023) ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions Exp Mol Med PMID: 36759578
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
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
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
Park et al (2018) Modulation of Protein Synthesis by eIF2α Phosphorylation Protects Cell from Heat Stress-Mediated Apoptosis. Cells 7 PMID: 30544621
Do you know of a great paper that uses GSK 2606414 from Tocris? Please let us know.
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