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Sephin1

Sephin-1 (NSC-65390) 是 holophosphatase 的选择性抑制剂,这是一种小分子,可在体内安全且选择性地抑制蛋白磷酸酶1的调节亚基。Sephin-1 可选择性地限制和抑制应激诱导的 PPP1R15A。

  • 货号:
    TK0532
  • 规格:
    1mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

CAS No.951441-04-6
生物活性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.
分子式C8H9N4Cl
分子量196.64
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder, -20°C ,3 years
溶解性数据DMSO : 50 mg/mL (254.27 mM; Need ultrasonic)
体内研究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.
体外研究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.
纯度及产品资料98%