Biological Activity of GSK2606414

GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.
IC50 Value: 0.4 nM [1]
Target:PERK
GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states [1]. It is implicated that PERK plays an important role in tumorigenesis and cancer cell survival.
 

References on GSK2606414

[1]. Axten JM, Medina JR, Feng Y, 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 Aug 23;55(16):7193-207.