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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.

Cat. No. Product Name CAS No. Information
H8528

MK-28

 		864388-65-8

MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
H2227

ISRIB trans-isomer

 		1597403-47-8

ISRIB trans-isomer is a potent inhibitor of PERK signaling, potently reverses the effects of eIF2α phosphorylation with IC50 of 5 nM; reduces the viability of cells subjected to PERK-activation by chronic endoplasmic reticulum stress, display significant enhancement in spatial and fear-associated learning; ISRIB is a potent inhibitor of the integrated stress response (ISR)integrated stress response (ISR), 100-fold more potent than cis-ISRIB (IC50=600 nM).
H2226

GSK-2606414

 		1337531-36-8

An orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM; inhibits PERK activation in cells and inhibits the growth of human tumor xenograft in mice; reduces p-eIF2α levels and enhanced novel taste learning and conditioned taste aversion, but not memory retrieval in rats.
H2225

CCT020312

 		324759-76-4

CCT020312 (CCT-020312) is a small molecule PERK activator, inhibits pRB phosphorylation in HT29 colon carcinoma cells with EC50 of 5.1 uM; shows no effect on the activity on CDK4/cyclin D or CDK1/cyclin B, effectively inhibits cell proliferation of HT29 colon carcinoma cells with IC50 of 3.1 uM (96 h); elicits EIF2A phosphorylation in cells, does not induce full ER stress signalling; also reduced tau phosphorylation, tau conformational change and 4-repeat tau isoforms, and increased cell viability in cultured human neurons, significantly improved memory and locomotor function, reduced tau pathology, and prevented dendritic spine and motoneuron loss in P301S tau mice.

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