ISRIB

製品コードS0706 バッチS070603

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式
C22H24Cl2N2O4
分子量 451.34 CAS No. 548470-11-7
Solubility (25°C)* 体外 DMSO 8 mg/mL (17.72 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 ISRIB is an integrated stress response (ISR) inhibitor that potently reverses the effects of eukaryotic initiation factor 2α (eIF2α) phosphorylation.
in vitro

ISRIB, an integrated stress response (ISR) inhibitor, reverses the effect of thapsigargin (TG) on translation, notably inhibits ER stress-induced cFLIP loss and prevents cFLIP levels down-regulation.[2]

in vivo

In an instability-induced intervertebral disc degeneration (IDD) model in mice, ISRIB suppressed p-eIF2α/ATF4/Ihh and prevented IDD via protecting the anti-oxidative enzymes and decreased the NP cell apoptosis.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116 cells
濃度 220 nM
反応時間 1 h
実験の流れ

HCT116 cells are pre-treated with ISRIB (220 nM) for 1 h prior TG treatment for the indicated times. To analyze protein synthesis, puromycin is added in the last 10 min of treatment and puromycin incorporation to the nascent protein chain is assessed by western blotting using an anti-puromycin antibody. Levels of both cFLIP isoforms are determined in whole cell extracts by western blotting and quantified.

動物実験 動物モデル C57 background BL/6J mice of intervertebral disc degeneration (IDD) models
投薬量 0.25 mg/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23741617/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8813907/
  • https://pubmed.ncbi.nlm.nih.gov/34164397/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

The integrated stress response drives MET oncogene overexpression in cancers [ EMBO J, 2025, 44(4):1107-1130] PubMed: 39774381
The role of vitamin K and its antagonist in the process of ferroptosis-damaged RPE-mediated CNV [ Cell Death Dis, 2025, 16(1):190] PubMed: 40108164
Combination of astragalus polysaccharide with Diosbulbin B exerts an enhanced antitumor effect in BRAFmut papillary thyroid cancer with decreased liver toxicity [ Cancer Cell Int, 2025, 25(1):245] PubMed: 40604967
Reduced EZH1/2 expression in imipridone-treated cells correlates with synergy following combinations with EZH1/2 or HDAC inhibitors in diffuse glioma and other tumors [ Am J Cancer Res, 2025, 15(3):1307-1320] PubMed: 40226473
PERK Regulates Epithelial-Mesenchymal Transition Through Autophagy and Lipid Metabolism in Lens Epithelial Cells [ Invest Ophthalmol Vis Sci, 2025, 66(5):35] PubMed: 40408092
NAD+ dependent UPRmt activation underlies intestinal aging caused by mitochondrial DNA mutations [ Nat Commun, 2024, 15(1):546] PubMed: 38228611
Nucleus pulposus cells regulate macrophages in degenerated intervertebral discs via the integrated stress response-mediated CCL2/7-CCR2 signaling pathway [ Exp Mol Med, 2024, 56(2):408-421.] PubMed: 38316963
A New Insight into the Mechanism of Atrazine-Induced Neurotoxicity: Triggering Neural Stem Cell Senescence by Activating the Integrated Stress Response Pathway [ Research (Wash D C), 2024, 7:0547] PubMed: 39679284
Deubiquitylase OTUD3 regulates integrated stress response to suppress progression and sorafenib resistance of liver cancer [ Cell Rep, 2024, 43(7):114487] PubMed: 38996071
GDF15 ameliorates sepsis-induced lung injury via AMPK-mediated inhibition of glycolysis in alveolar macrophage [ Respir Res, 2024, 25(1):201] PubMed: 38725041

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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