Raphin1 acetate is a selective inhibitor of PPP1R15B (R15B) and bound strongly (Kd value of 0.033 μM) to the R15B-PP1c holophosphatase. Moreover, Raphin1 acetate was ~30-fold selective in binding R15B-PP1c over R15A-PP1c and did not bind to PP1c. In cells, Raphin1 acetate caused a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis. In vitro, Raphin1 acetate inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment. Raphin1 acetate was orally bioavailable, crossed the blood-brain barrier, and demonstrated efficacy in a mouse model of Huntington’s disease. This product is also available as the free base (Axon 3004)

KEYWORDS: Raphin1 acetate | supplier | PPP1R15B (R15B) inhibitor | Raphin 1 acetate | Raphin-1 acetate | CAS [2242616-04-0] | [2022961-17-5] | Non Selective (Serine-Threonine and Tyrosine Specific Phosphodiesters) | PPP1R15B | Inhibitor | Enzymes | Huntington’s disease