SALUBRINAL

Description

Salubrinal is a selective phosphatase inhibitor that prevents dephosphorylation of eukaryotic translation initiation factor 2 subunit α (eIF_2α), protecting PC12 cells from endoplasmic reticulum stress-mediated apoptosis (EC₅₀ = 15 μM). It appears to block the action of protein phosphatase 1 (PP1) on eIF_2α 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 eIF_2α. As eIF_2α has a role in bone formation, salubrinal is being studied for its effects in osteoporosis.

The Uses of SALUBRINAL

Salubrinal is an endoplasmic reticulum stress blocker that modulates sleep homeostasis and activation of sleep- and wake-regulatory neurons

The Uses of SALUBRINAL

Salubrinal is a selective Inhibitor of eIF2α (eukaryotic translation initiation factor 2 α-subunit) dephosphorylation, inhibiting global protein translation. Salubrinal is a specific inhibitor of ER Stress induced apoptosis.

The Uses of SALUBRINAL

Salubrinal has been used to study the effect of stress-protective genes and pathways on organism development and lifespan. It has also been used to study the therapeutic potential of salubrinal in methamphetamine induced blood–brain barrier disruption.

What are the applications of Application

Salubrinal is a cell permeable and selective inhibitor of eIF-2α used to study ER stress-induced apoptosis.

Definition

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).

Biological Activity

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).

Biochem/physiol Actions

Salubrinal is a selective Inhibitor of eIF2α (eukaryotic translation initiation factor 2 α-subunit) dephosphorylation, inhibiting global protein translation. Salubrinal is a specific inhibitor of ER Stress induced apoptosis.

Storage

+4°C

References

1) Boyce?et al. (2005)?A selective inhibitor of eIF2α dephosphorylation protects cells from ER stress; Science,?307?935 2) Kessel (2006)?Protection of Bcl-2 by salubrinal; Biochem. Biophys. Res. Commun.,?346?1320 3) He?et al. (2013)?Osteoporosis regulation by salubrinal through eFI27alpha; mediated differentiation of osteoclast and osteoblast; Cell. Signal.,?25?552