所有图片(1)
About This Item
经验公式（希尔记法）:
C8H9ClN4
CAS号:
分子量:
196.64
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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品質等級
化驗
≥95% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
NC(N/N=C/C1=CC=CC=C1Cl)=N
InChI
1S/C8H9ClN4/c9-7-4-2-1-3-6(7)5-12-13-8(10)11/h1-5H,(H4,10,11,13)/b12-5+
InChI 密鑰
PDWJALXSRRSUHR-LFYBBSHMSA-N
生化／生理作用
利用小鼠模型进行的体内研究表明，sephin1通过阻止eIF2α（真核起始因子2）去磷酸化抑制神经变性。
Sephin1 是一种全磷酸酶的选择性抑制剂。它是一种胍贝兹衍生物，能结合并抑制应激诱导蛋白磷酸酶 1 (PPP1R15A) 的一个调节亚基，但不抑制组成型 PPP1R15B，且缺乏 α2-肾上腺素能活性。真核翻译起始因子 2 的eIF2α, α 的磷酸化，减少蛋白质合成，防止内质网 (ER) 中错误折叠蛋白质的积累。PPP1R15A 招募丝氨酸/苏氨酸蛋白磷酸酶 PP1 去磷酸化 eIF2α因此抑制 PPP1R15A 活性延长 eIF2α 的磷酸化并帮助其防止错误折叠蛋白的积累。 体外 Sephin1 保护细胞免受致死蛋白错误折叠和细胞毒性内质网应激的影响。体内 sephin1 预防了小鼠中两种不相关的蛋白错误折叠疾病（腓骨肌萎缩症 1B 和 ALS）。
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
PPP1R15A-mediated dephosphorylation of eIF2α is unaffected by Sephin1 or Guanabenz.
Crespillo-Casado A, et al.
eLife, 6, e26109-e26109 (2017)
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Identification of new mechanisms mediating insulin sensitivity is important to allow validation of corresponding therapeutic targets. In this study, we first used a cellular model of skeletal muscle cell iron overload and found that endoplasmic reticulum (ER) stress and insulin
Nadejda Capatina et al.
The Journal of physiology, 599(17), 4153-4181 (2021-07-17)
Endoplasmic reticulum (ER) stress promotes placental dysmorphogenesis and is associated with poor pregnancy outcomes. We show that unfolded protein response signalling pathways located in the ER drive differentiation of mouse trophoblast stem cells into trophoblast subtypes involved in development of
Juliette Humeau et al.
Cell death & disease, 11(6), 433-433 (2020-06-10)
The integrated stress response is characterized by the phosphorylation of eukaryotic initiation factor-2α (eIF2α) on serine 51 by one out of four specific kinases (EIF2AK1 to 4). Here we provide three series of evidence suggesting that macroautophagy (to which we
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