SALUBRINAL Chemical Properties

Melting point:

>160°C (dec.)

Density 

1.474±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

10.70±0.70(Predicted)

color 

white to light yellow to light gray

Water Solubility 

Insoluble in water.

Sensitive 

Light Sensitive

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26

WGK Germany 

3

SALUBRINAL Usage And Synthesis

Description

Selective eukaryotic translation initiation factor 2 subunit α (elF2α) dephosphorylation inhibitor. Salubrinal is a selective Inhibitor of eIF2α (eukaryotic translation initiation factor 2 α-subunit) dephosphorylation, and is primarily used experimentally, to study stress responses in eukaryotic cells associated with the action of eIF2. Salubrinal indirectly inhibits eIF2 as a result of reduced dephosphorylation of its α-subunit resulting in activation of stress response pathways usually triggered by events such as oxidative stress or buildup of unfolded protein in the endoplasmic reticulum. Salubrinal can protect PC12 cells from endoplasmic reticulum stress-mediated apoptosis (EC50 = 15 μM) and prevent replication of herpes virus (IC50 = 3 μM), by inhibiting dephosphorylation of eIF2α. As eIF2α has a role in bone formation, salubrinal is also being studied for its effects in osteoporosis. Besides, it also shows potential neuroprotective actions. Although salubrinal has putative therapeutic value due to its function, it is as yet only used experimentally.

References

1. https://en.wikipedia.org/wiki/Salubrinal
2. http://www.sigmaaldrich.com/catalog/product/sigma/sml0951?lang=en&region=CA
3. https://www.tocris.com/dispprod.php?ItemId=143907#.WQfadeyECP0
4. http://www.selleckchem.com/products/salubrinal.html
5. https://www.caymanchem.com/product/14735
6. https://www.hellobio.com/salubrinal.html

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.

Uses

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.

Uses

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

Uses

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.

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

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