SEPHIN1

SEPHIN1

Stock Code: 3574797
Manufacturer Part No: SML1356-10MG
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Biochem/physiol Actions


In vivo studies using mice models show that sephin1 suppresses neurodegeneration, by preventing eIF2? (eukaryotic initiation factor 2) dephosphorylation.


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).


Packaging


10 mg in glass bottle

Colourwhite to beige
Quality Level100
InChI keyPDWJALXSRRSUHR-LFYBBSHMSA-N
InChI1S/C8H9ClN4/c9-7-4-2-1-3-6(7)5-12-13-8(10)11/h1-5H,(H4,10,11,13)/b12-5+
ManufacturerSIGMA-ALDRICH
SolubilityDMSO: 20 mg/mL, clear
Formpowder
Assay≥95% (HPLC)

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