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cis-ISRIB is a weak inhibitor of PERK signaling compared to trans-ISRIB , potently reverses the effects of eIF2α phosphorylation with IC50 of 600 nM.ISRIB reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress, displays significant enhancement in spatial and fear-associated learning.ISRIB is a potent inhibitor of the integrated stress response (ISR)integrated stress response (ISR).
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
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