-
説明
Salubrinal is a selective phosphatase inhibitor that prevents dephosphorylation of eukaryotic translation initiation factor 2 subunit α (eIF2α), protecting PC12 cells from endoplasmic reticulum stress-mediated apoptosis (EC50 = 15 μM). It appears to block the action of protein phosphatase 1 (PP1) on eIF2α although it does not mimic calyculin A, another PP1-selective inhibitor, in toxicity or phosphorylation pattern. Salubrinal also prevents replication of herpes virus (IC50 = 3 μM), by inhibiting dephosphorylation of eIF2α. As eIF2α has a role in bone formation, salubrinal is being studied for its effects in osteoporosis.
-
使用
Salubrinal is an endoplasmic reticulum stress blocker that modulates sleep homeostasis and activation of sleep- and wake-regulatory neurons
-
定義
ChEBI: A member of the class of quinolines that is a mixed aminal resulting from the formal condensation oftrichloroacetaldehyde with the amide nitrogen of trans-cinnamamide and the primary amino group of 1-quinolin-8-ylthiourea. It is a selective in
ibitor of cellular complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit alpha (eIF2alpha).
-
生物活性
Cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2 α ). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC 50 ~ 15 μ M).
