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Cell Cycle/DNA Damage——PERK

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. PERK is highly expressed in pancreatic beta-cells and is essential in the beta-cell's development, differentiation and function.

PERK is a type I ER membrane protein containing a stress-sensing domain facing the ER lumen, a transmembrane segment, and a cytosolic kinase domain. Increase in unfolded proteins in the ER causes release of ER chaperones from the stress-sensing domain of PERK, which results in its activation via oligomerization and autophosphorylation at multiple serine, threonine, and tyrosine residues. Upon activation, PERK phosphorylates eIF2α at serine 51, rendering it an inhibitor of the ribosome translation initiation complex, consequently reducing overall protein synthesis. The reduction in translation reduces the ER burden, providing time for the cell to process or degrade the accumulated unfolded proteins to restore ER homeostasis. Although global protein synthesis is decreased, there is specific increased translation of certain mRNAs, such as ATF4, which modulate cellular survival pathways and enhance UPR function. Interfering with PERK function in cancer cells may limit their ability to thrive under hypoxia or nutrient deprived conditions and lead to apoptosis or tumor growth inhibition.

Cell Cycle/DNA Damage——PERK(6)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM8549 AMG PERK 44

AMG PERK 44 是一种口服有效的,高选择性的 PERK 抑制剂,IC50 为 6 nM。AMG PERK 44 对 PERK 的选择性分别是 GCN2 (IC50=7300 nM) 和 B-Raf (IC50 >1000 nM) 的 1000 倍和 160 倍。AMG PERK 44 可以诱导自噬 (autophagy)。

1883548-84-2 99%
KM6554 CCT020312

CCT020312 是选择性的 EIF2AK3/PERK 的激活剂。CCT020312 可诱导细胞细胞中 EIF2A 的磷酸化。

324759-76-4 98%
KM15073 GSK2606414

GSK2606414 是可渗透细胞且有口服活性的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂,IC50值为 0.4 nM。

1337531-36-8 99%
KM7951 GSK2656157

GSK2656157 是选择性,ATP竞争性的 PERK 抑制剂,IC50 值为 0.9 nM。

1337532-29-2 99%
KM3043 ISRIB (trans-isomer)

ISRIB (trans-isomer)是高效的PERK抑制剂,IC50值为 5 nM。ISRIB 可有效逆转 eIF2α 磷酸化的作用 (IC50=5 nM)。

1597403-47-8 99%
KM7633 MK-28

MK-28 是有效、选择性的 PERK 激动剂。MK-28 在小鼠中表现出良好的药代动力学特征,且能透过血脑屏障。

864388-65-8 99%
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