Sephin1 是一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物,是一种磷酸酶调节亚单位PPP1R15A (R15A)的选择性抑制剂。它能够抑制 eIF2α 去磷酸化,从而延长保护反应。它具有抗朊病毒作用。
产品描述
Sephin1 is a selective inhibitor of holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo.
体外活性
Sephin1 dose and time dependently reduced PrPSc in different neuronal cell lines which were persistently infected with various prion strains. In addition, prion seeding activity was reduced in Sephin1-treated cells. Importantly, we found that Sephin1 significantly overcame the endoplasmic reticulum (ER) stress induced in treated cells, as measured by lower expression of stress-induced aberrant prion protein[1].
体内活性
In a mouse model of prion infection, intraperitoneal treatment with Sephin1 significantly prolonged survival of prion-infected mice. When combining Sephin1 with the neuroprotective drug metformin, the survival of prion-infected mice was also prolonged[1].
Cas No.
951441-04-6
分子式
C8H9ClN4
分子量
196.64
别名
lcerguastat;IFB-088;Sephin 1
储存和溶解度
DMSO:200mg/ml(1017.10mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years