405060-95-9 Usage
Description
Salubrinal is a selective eukaryotic translation initiation factor 2 subunit α (eIF2α) dephosphorylation inhibitor. It is a mixed aminal resulting from the formal condensation of trichloroacetaldehyde with the amide nitrogen of trans-cinnamamide and the primary amino group of 1-quinolin-8-ylthiourea. Salubrinal is primarily used experimentally to study stress responses in eukaryotic cells associated with the action of eIF2. It indirectly inhibits eIF2 as a result of reduced dephosphorylation of its α-subunit, resulting in the activation of stress response pathways usually triggered by events such as oxidative stress or the buildup of unfolded protein in the endoplasmic reticulum.
Uses
Used in Research Applications:
Salubrinal is used as a research tool for studying the effect of stress-protective genes and pathways on organism development and lifespan. It is also used to investigate the therapeutic potential of salubrinal in methamphetamine-induced blood-brain barrier disruption.
Used in Pharmaceutical Applications:
1. Salubrinal is used as an endoplasmic reticulum stress blocker that modulates sleep homeostasis and activation of sleepand wake-regulatory neurons.
2. Salubrinal is used as a specific inhibitor of ER Stress induced apoptosis, protecting PC12 cells from endoplasmic reticulum stress-mediated apoptosis (EC50 = 15 μM) and preventing replication of herpes virus (IC50 = 3 μM) by inhibiting dephosphorylation of eIF2α.
Used in Osteoporosis Research:
Salubrinal is being studied for its effects in osteoporosis, as eIF2α has a role in bone formation.
Used in Neuroprotective Research:
Salubrinal also shows potential neuroprotective actions and is being investigated for its therapeutic value in this area.
References
1. https://en.wikipedia.org/wiki/Salubrinal
2. http://www.sigmaaldrich.com/catalog/product/sigma/sml0951?lang=en®ion=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
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
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.
Check Digit Verification of cas no
The CAS Registry Mumber 405060-95-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,0,5,0,6 and 0 respectively; the second part has 2 digits, 9 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 405060-95:
(8*4)+(7*0)+(6*5)+(5*0)+(4*6)+(3*0)+(2*9)+(1*5)=109
109 % 10 = 9
So 405060-95-9 is a valid CAS Registry Number.
InChI:InChI=1/C21H17Cl3N4OS/c22-21(23,24)19(27-17(29)12-11-14-6-2-1-3-7-14)28-20(30)26-16-10-4-8-15-9-5-13-25-18(15)16/h1-13,19H,(H,27,29)(H2,26,28,30)/b12-11+
