Raphin1 acetate 是具有口服活性的、可透过血脑屏障的、选择性调节性磷酸酶PPP1R15B 抑制剂。它与 R15B-PP1c 全磷酸酶强烈结合 (Kd=33 nM)，与 R15A-PP1c 相比，结合 R15B-PP1c 约为其 30 倍的选择性。它可减少蛋白质错误折叠疾病的小鼠模型中的生物和分子缺陷。

Raphin1 acetate is a selective and orally bioavailable regulatory phosphatase PPP1R15B (R15B) inhibitor.

Raphin1, a selective inhibitor of R15B.?In cells, Raphin1 caused a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis.?In vitro, Raphin1 inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment.

Raphin1 was orally bioavailable, crossed the blood-brain barrier, and demonstrated efficacy in a mouse model of Huntington's disease.

2242616-04-0

C10H12Cl2N4O2

291.13

DMSO:40 mg/mL (137.4 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years