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。
产品描述
Raphin1 acetate is a selective and orally bioavailable regulatory phosphatase PPP1R15B (R15B) inhibitor.
体外活性
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.
体内活性
Raphin1 was orally bioavailable, crossed the blood-brain barrier, and demonstrated efficacy in a mouse model of Huntington's disease.
Cas No.
2242616-04-0
分子式
C10H12Cl2N4O2
分子量
291.13
储存和溶解度
DMSO:40 mg/mL (137.4 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years