GSK2606414

GSK2606414 is a potent, selective, and orally available small molecule inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), also known as eukaryotic translation initiation factor 2 alpha kinase 3 (EIF2AK3). It was the first selective inhibitor discovered for PERK and demonstrates good oral bioavailability and blood-brain barrier penetration. PERK is a key mediator of the unfolded protein response pathway, which regulates protein synthesis in response to endoplasmic reticulum stress—a process implicated in cancer and neurodegenerative diseases such as prion disease and Alzheimer's disease. Preclinical studies have shown that GSK2606414 can be neuroprotective in animal models by preventing cognitive deficits associated with prion disease; however, it does not extend lifespan in these models. Notable side effects include weight loss and hyperglycemia due to inhibition of pancreatic PERK activity[1][6][8].

Other names

PERK Inhibitor I