Sephin1 is a selective inhibitor of a holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo. Sephin1 selectively bound and inhibited the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress. In vivo, Sephin1 safely prevented the motor, morphological, and molecular defects of two otherwise unrelated protein-misfolding diseases in mice, Charcot-Marie-Tooth 1B, and amyotrophic lateral sclerosis. Sephin1may have potential to safely prevent two protein misfolding diseases.
CAS Number: 951441-04-6
Molecular Weight: 258.66
Chemical Name: (E)-2-(2-chlorobenzylidene)hydrazine-1-carboximidamide carbonic acid salt
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Sephin1 was used at 0.1-1 µM final concentration in vitro and in cellular assays.
Sephin1 was orally dosed to MPZmutant mice or SOD1mutant mice at 1 mg/Kg twice a day.
- Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. (2015) Science. 348(6231):239-42.
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