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2022961-17-5

2022961-17-5 structure
2022961-17-5 structure
  • Name: Raphin 1
  • Chemical Name: Raphin1
  • CAS Number: 2022961-17-5
  • Molecular Formula: C8H8Cl2N4
  • Molecular Weight: 231.08
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
  • Create Date: 2019-10-06 16:20:52
  • Modify Date: 2024-01-02 18:32:15
  • Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].

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

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

In Vitro Raphin1 causes a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis[1]. Raphin1 inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment[1].
In Vivo Raphin1 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 also decreases SDS-insoluble huntingtin assemblies and nuclear inclusions in the cortex of HD82Q mice[1].
References

[1]. Krzyzosiak A, et al. Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B. Cell. 2018 Aug 23;174(5):1216-1228.e19.

Molecular Formula C8H8Cl2N4
Molecular Weight 231.08
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