1. Cell Cycle/DNA Damage
  2. PERK

PERK

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. PERK is implicated in tumorigenesis and cancer cell survival. GSK2606414 is an orally available, potent, and selective PERK inhibitor. GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. PERK activation is independent of the large increase in unfolded nascent proteins within the ER following transient global brain ischemia.

PERK Related Products (3):

Cat. No. Product Name Effect Purity
  • HY-18072
    GSK2606414 Inhibitor 99.38%
    GSK2606414 is an orally available and selective PERK inhibitor with an IC50 of 0.4 nM.
  • HY-13820
    GSK2656157 Inhibitor 99.66%
    GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 value of 0.9 nM, and highly selective for PERK with IC50 values of > 100 nM against a panel of 300 kinases.
  • HY-12495
    ISRIB trans-isomer Inhibitor >98.0%
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.