2242616-04-0
2242616-04-0 structure
- Name: Raphin1 acetate
- Chemical Name: Raphin1 acetate
- CAS Number: 2242616-04-0
- Molecular Formula: C10H12Cl2N4O2
- Molecular Weight: 291.13
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
- Create Date: 2019-10-07 09:09:11
- Modify Date: 2024-01-04 00:19:51
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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].
| Name | Raphin1 acetate |
|---|---|
| Synonyms | MFCD32201062 |
| 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Molecular Formula | C10H12Cl2N4O2 |
|---|---|
| Molecular Weight | 291.13 |