Sephin 1 Property

Boiling point:

320.9±44.0 °C(Predicted)

Density 

1.35±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble in DMSO (100 mM)

form 

powder

pka

8.74±0.30(Predicted)

color 

white to beige

Safety

RIDADR 

UN 2811 6.1 / PGIII

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Sephin 1 Chemical Properties,Usage,Production

Uses

Sephin 1 is a selective inhibitor of holophosphatase, a regulatory subunit of protein phosphatase 1. May be used in the prevention of protein misfolding diseases.

Biochem/physiol Actions

Sephin1 is a selective inhibitor of a holophosphatase. It is a guanabez derivative that binds to and inhibits a regulatory subunit of the stress-induced protein phosphatase 1 (PPP1R15A), but not the constitutive PPP1R15B, and lacks α2-adrenergic activity. Phosphorylation of eIF2α, α subunit of eukaryotic translation initiation factor 2, reduces protein synthesis and prevents the accumulation of misfolded protein in the endoplasmic reticulum (ER). PPP1R15A recruits the serine/threonine-protein phosphatase PP1 to dephosphorylate eIF2α, so inhibiting PPP1R15A activity prolongs the phosphorylation of eIF2α and aids in its prevention of the accumulation of misfolded protein. In vitro Sephin1 protected cells from lethal protein misfolding and cytotoxic ER stress. In vivo sephin1 prevented two unrelated protein misfolding diseases in mice (Charchot-Marie-Tooth 1B and ALS).

storage

+4°C