Icerguastat (Sephin1) ，一种缺乏 α2-肾上腺素能活性的 Guanabenz 衍生物，是磷酸酶调节亚单位 PPP1R15A (R15A) 的选择性抑制剂。Icerguastat 抑制 eIF2α 去磷酸化，从而延长保护反应。Icerguastat 具有抗朊病毒作用。

Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect.

Solid

Icerguastat (5 μM) prolongs eIF2α phosphorylation in oligodendrocytes under stress.
Icerguastat (Sephin1) (selective inhibitor of a holophosphatase), safely and selectively inhibits a regulatory subunit of protein phosphatase 1 in vivo. Sephin1 selectively binds and inhibits the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress. has not independently confirmed the accuracy of these methods. They are for reference only.

Icerguastat (4-8 mg/kg; i.p.; daily for 35 days) delays the onset of EAE (experimental autoimmune encephalomyelitis).
Icerguastat (100 μg; i.p.) prolongs the survival of prion-infected mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Chen Y, et al. Sephin1, which prolongs the integrated stress response, is a promising therapeutic for multiple sclerosis. Brain. 2019;142(2):344-361.
[2]. Das I, et al. Preventing proteostasis diseases by selective inhibition of a phosphatase regulatory subunit. Science. 2015;348(6231):239-242.
[3]. Thapa S, et

In Vitro: DMSO : 50 mg/mL (254.27 mM; Need ultrasonic)配制储备液