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

PERK (蛋白激酶R样内质网激酶)

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 相关产品 (4):

目录号 产品名 作用方式 纯度
  • HY-13820
    GSK2656157 Inhibitor 99.66%
    GSK2656157 是选择性,ATP竞争性的 PERK 抑制剂,IC50 值为 0.9 nM。
  • HY-119240
    CCT020312 Activator 98.97%
    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。
  • HY-12661A
    AMG PERK 44 Inhibitor ≥99.0%
    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)。
  • HY-137207
    MK-28 Activator 99.50%
    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。
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