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Merck
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Key Documents

SML0843

Sigma-Aldrich

ISRIB

≥98% (HPLC), powder, integrated stress response inhibitor

同義詞:

反式-N,N′-1,4-环己烷二基双 \ [2-(4-氯苯氧基)-乙酰胺, 反式-N,N′-(环己烷-1,4-二基)双(2-(4-氯苯氧基)乙酰胺, 整合应激反应抑制剂

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About This Item

經驗公式(希爾表示法):
C22H24Cl2N2O4
CAS號碼:
分子量::
451.34
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

product name

ISRIB, ≥98% (HPLC)

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 1 mg/mL, clear (warmed)

儲存溫度

2-8°C

SMILES 字串

ClC1=CC=C(OCC(N[C@@H]2CC[C@@H](NC(COC3=CC=C(Cl)C=C3)=O)CC2)=O)C=C1

InChI

1S/C22H24Cl2N2O4/c23-15-1-9-19(10-2-15)29-13-21(27)25-17-5-7-18(8-6-17)26-22(28)14-30-20-11-3-16(24)4-12-20/h1-4,9-12,17-18H,5-8,13-14H2,(H,25,27)(H,26,28)/t17-,18-

InChI 密鑰

HJGMCDHQPXTGAV-IYARVYRRSA-N

應用

ISRIB(综合应激反应抑制剂)已被用作综合应激反应的抑制剂。

生化/生理作用

ISRIB 是一种血脑屏障渗透剂,是内质网应激适应性受损的有效选择性综合应激反应 (ISR) 抑制剂。ISRIB 是 PERK 信号的有效抑制剂,可有效逆转 eIF2a 磷酸化作用,恢复细胞翻译能力。ISRIB 增强啮齿类动物的认知记忆。
ISRIB(综合应激反应抑制剂)作为一种药物,赋予细胞抵抗真核起始因子2(eIF2)α磷酸化(如激活转录因子4(ATF4)和真核翻译起始因子4E(eIF4E)结合)的下游作用的抗性 蛋白质1(4E-BP1)诱导。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Ting Zhang et al.
The Journal of pharmacology and experimental therapeutics, 378(3), 197-206 (2021-07-04)
Phosphorylation of the eukaryotic translation initiation factor 2 α-subunit, which subsequently upregulates activating transcription factor 4 (ATF4), is the core event in the integrated stress response (ISR) pathway. Previous studies indicate phosphorylation of eukaryotic translation initiation factor 2 ɑ-subunit in
B Balakrishnan et al.
Biochimica et biophysica acta. Molecular basis of disease, 1865(11), 165516-165516 (2019-07-31)
Loss of galactose-1 phosphate uridylyltransferase (GALT) activity in humans results in Classic Galactosemia, and the GalT-deficient (GalT-/-) mouse mimics the patient condition. GalT-/- ovaries display elevated endoplasmic reticulum (ER) stress marker, BiP, and downregulated canonical phosphatidylinositol 3-kinase (Pi3k)/protein kinase B
Z D Kabir et al.
Molecular psychiatry, 22(8), 1096-1109 (2017-06-07)
CACNA1C, encoding the Ca
Caitlin M Rodriguez et al.
Nature neuroscience, 23(3), 386-397 (2020-02-19)
Repeat-associated non-AUG-initiated translation of expanded CGG repeats (CGG RAN) from the FMR1 5'-leader produces toxic proteins that contribute to neurodegeneration in fragile X-associated tremor/ataxia syndrome. Here we describe how unexpanded CGG repeats and their translation play conserved roles in regulating
Joni Vanneste et al.
Biomedicines, 10(5) (2022-05-29)
Stress granules are non-membrane bound granules temporarily forming in the cytoplasm in response to stress. Proteins of the nucleocytoplasmic transport machinery were found in these stress granules and it was suggested that stress granules contribute to the nucleocytoplasmic transport defects

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