1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. PERK

PERK

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is a type I endoplasmic reticulum transmembrane protein containing a stress-sensing domain facing the endoplasmic reticulum lumen and a cytosolic kinase domain. PERK is a major component of the unfolded protein response (UPR), which promotes the adaptation of cells to various forms of stress. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.

PERK regulates proliferation of beta cells during embryonic and neonatal development and is essential for viability of acinar cells in mouse exocrine pancreas, neither of which is associated with endoplasmic reticulum stress response. PERK is also required for endoplasmic reticulum functions including proinsulin trafficking and quality control in beta cells. Similarly, PERK modulates proliferation and differentiation of osteoblasts as well as secretion of type I collagen.

PERK phosphorylates α subunit of the translation initiation factor eIF2 at serine 51, a modification that plays a key role in the regulation of mRNA translation in stressed cells. PERK-eIF2α phosphorylation pathway maintains insulin biosynthesis and glucose homeostasis, facilitates tumor formation and decreases the efficacy of tumor treatment with chemotherapeutic drugs.

PERK Related Products (4):

Cat. No. Product Name Effect Purity
  • HY-18072
    GSK2606414 Inhibitor 99.38%
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
  • HY-13820
    GSK2656157 Inhibitor 99.66%
    GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
  • HY-12495
    ISRIB (trans-isomer) Inhibitor 99.37%
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.
  • HY-119240
    CCT020312 Activator 98.56%
    CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
Isoform Specific Products

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