1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. Raphin1 acetate

Raphin1 acetate 

Cat. No.: HY-123960A
Handling Instructions

Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.

For research use only. We do not sell to patients.

Raphin1 acetate Chemical Structure

Raphin1 acetate Chemical Structure

CAS No. : 2242616-04-0

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Description

Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].

IC50 & Target

Kd: 33 nM (R15B-PP1c holophosphatase)[1]

In Vitro

Raphin1 acetate causes a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis[1].
Raphin1 acetate inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment[1].

In Vivo

Raphin1 acetate improves weight of HD82Q mice treated from 4 to ∼10 weeks of age with 2 mg/kg of Raphin1 once a day by oral gavage. Raphin1 acetate also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice[1].

Molecular Weight

291.13

Formula

C₁₀H₁₂Cl₂N₄O₂

CAS No.

2242616-04-0

SMILES

N=C(N/N=C/C1=CC=CC(Cl)=C1Cl)N.CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Raphin1 acetate
Cat. No.:
HY-123960A
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