GSK 2606414

Key Product Details

Product Description

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

Product Specifications for GSK 2606414

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 71 publications citing the usage of this product.

• Harding Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 2012 PMID: 23148209
• Axten 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. 2012 PMID: 22827572

Product Documents for GSK 2606414