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Biological Activity:
GSK2606414 is an orally available, potent, and selective PERK inhibitor. Compound 38 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:
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.
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C16169 GSK2606414 (1337531-36-8)