Raphin1

Cas No.:	2022961-17-5
Chemical Name:	(E)-2-(2,3-dichlorobenzylidene)hydrazine-1-carboximidamide
Synonyms:	Raphin1,Raphin 1,Raphin-1,phosphatase inhibitor, PPP1-R15B inhibitor
SMILES:	N(C(N)=N)/N=C/C1=CC=CC(Cl)=C1Cl
Formula:	C8H8Cl2N4
M.Wt:	230.01
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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].
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].