GSK 2606414

Cat. No. 5107

GSK 2606414 C24H20F3N5O [1337531-36-8]

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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

Biological Activity

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

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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Keywords: GSK 2606414, supplier, GSK2606414, potent, selective, protein, kinase, R-like, ER, kinase, PERK, orally, bioavailable, antitumor, ER-stress, Tocris Bioscience, PERK Inhibitor products

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