| Identification | Back Directory | [Name]
Raphin1 | [CAS]
2022961-17-5 | [Synonyms]
Raphin1
PPP1-R15B inhibitor
phosphatase inhibitor
(2E)-2-[(2,3-Dichlorophenyl)methylene]hydrazinecarboximidamide
Hydrazinecarboximidamide, 2-[(2,3-dichlorophenyl)methylene]-, (2E)-
RAPHIN1;RAPHIN 1;RAPHIN-1;PHOSPHATASE INHIBITOR; PPP1-R15B INHIBITOR | [Molecular Formula]
C8H8Cl2N4 | [MDL Number]
MFCD03653280 | [MOL File]
2022961-17-5.mol | [Molecular Weight]
231.08 |
| Chemical Properties | Back Directory | [Boiling point ]
360.1±52.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (540.94 mM) | [form ]
Solid | [pka]
8.37±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [storage]
Store at -20°C | [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. DOI:10.1016/j.cell.2018.06.030 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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