化合物Raphin1 acetate T8519

Product Introduction
Bioactivity


英文名: Raphin1 acetate

描述: 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。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 40 mg/mL (137.4 mM)


关键字: Raphin1 | Phosphatase | Raphin-1 acetate | Raphin-1 | Raphin1 acetate | Raphin 1 | Raphin1 Acetate | inhibit | Inhibitor

相关产品: Stearic acid | BN82002 | AS1949490 | Anticancer agent 144 | PTPσ Inhibitor, ISP | KY-226 | LUPENONE | Abyssinone V | MLS000544460 | Sodium etidronate

相关库: Glycometabolism Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Phosphatase Inhibitor Library | CNS-Penetrant Compound Library | Inhibitor Library | Metabolism Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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