Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is one of four known kinases that respond to cellular stress by deactivating the eukaryotic initiation factor 2 α (eIF2α) or other signal transduction cascades.In order for pancreatic beta-cells to develop, differentiate, and perform properly, PERK must be highly expressed in those cells.
A type I ER membrane protein called PERK has a transmembrane segment, a cytosolic kinase domain, and a stress-sensing domain that faces the ER lumen. The stress-sensing domain of PERK releases ER chaperones in response to an increase in unfolded proteins in the ER, which activates PERK via oligomerization and autophosphorylation at numerous serine, threonine, and tyrosine residues.When PERK is activated, it phosphorylates eIF2 at serine 51, turning it into an inhibitor of the ribosome translation initiation complex and lowering total protein synthesis as a result. The ER burden is lessened by the decrease in translation, giving the cell more time to process or degrade the accumulating unfolded proteins and reestablish ER homeostasis. Although there is a reduction in overall protein synthesis, there is a specific increase in the translation of some mRNAs, such as ATF4, which affect cellular survival pathways and improve UPR activity. Cancer cells may experience apoptosis or tumor growth inhibition if their ability to thrive in hypoxic or nutrient-deficient environments is inhibited by PERK function.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V17165 | BTdCPU | 1257423-87-2 | BTdCPU is an activator of HRI (heme-regulated eIF2α kinase) with anticancer activity. |
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V52038 | GSK143 dihydrochloride | 2341796-81-2 | GSK143 di-HCl is an orally bioactive, selective inhibitor of spleen tyrosine kinase (SYK) with pIC50 of 7.5. |
|
V0059 | GSK2606414 | 1337531-36-8 | GSK2606414 is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with an IC50 of 0.4 nM and at least 100-fold selectivity over the other EIF2AKs tested. |
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V75798 | HC-5404 | 2247396-91-2 | HC-5404 is a potent and specific PERK inhibitor. |
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V0061 | ISRIB (trans-isomer) | 1597403-47-8 | ISRIB, the trans-isomer of ISRIB, is a novel, potent and selective inhibitor of PERK (PRKR-like endoplasmic reticulum kinase or protein kinase R (PKR)-like endoplasmic reticulum kinase) with IC50 of 5 nM. |
|
V41189 | MK-28 | 864388-65-8 | MK-28 is a potent and specific PERK agonist. |
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V41095 | NSC 295642 | 77111-29-6 | NSC 295642 is a phosphatase inhibitor. |
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V53131 | PERK-IN-4 | 1337531-89-1 | PERK-IN-4 is a potent and specific PERK inhibitor (antagonist) with an IC 50 value of 0.3 nM. |
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V81087 | PERK-IN-4-d3 | PERK-IN-4-d3 is the deuterium labelled form of PERK-IN-4. | |
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V25179 | PERK-IN-6 | 1337532-14-5 | PERK-IN-6 (Compound 5) is a PERK inhibitor (antagonist) with IC50 of 2.5 nM. |
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