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SML1356 Sigma-Aldrich

Sephin1

≥95% (HPLC)

Synonym: (E)-2-(2-Chlorobenzylidene)hydrazinecarboximidamide, Sephin 1

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Gene Regulation and Expression,
InChI Key   PDWJALXSRRSUHR-LFYBBSHMSA-N
assay   ≥95% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 20 mg/mL, clear
storage temp.   2-8°C

Description

Packaging

10 mg in glass bottle

Biochem/physiol Actions

In vivo studies using mice models show that sephin1 suppresses neurodegeneration, by preventing eIF2α (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).

Safety & Documentation

Safety Information

RIDADR 
UN 2811 6.1 / PGIII

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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