4μ8C

製品コードS7272 バッチS727201

印刷

化学情報

Chemical Structure Synonyms IRE1 Inhibitor III Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H8O4
分子量 204.18 CAS No. 14003-96-4
Solubility (25°C)* 体外 DMSO 19 mg/mL (93.05 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 4μ8C (IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
in vitro

4μ8C blocks substrate(RIDD) access to the active site of IRE1 and selectively inactivates both Xbp1 splicing and IRE1-mediated mRNA degradation. IRE1 inhibition subsequently induces ER stress without measureable acute toxicity. [1]

4μ8C, as an IRE1 inhibitor, blocks IL-4, IL-5, and IL-13 production from CD4+ T cells. [2]
in vivo

4μ8c is an IRE1 Inhibitor III that reduces atherosclerotic lesion and effectively mitigate plaque development in mice.
特徴 IRE1 Rnase-selective inhibitor, used as a platform for developing new locally acting drugs.

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro IRE1 RNase and RIDD Assays
Analysis of radiolabeled Xbp1 substrate cleavage is performed as previously except that mammalian IRE1 reaction buffer is used. In vitro RIDD substrates are synthesized by in vitro transcription using the T7-MAXIscript Kit in the presence of 32P ATP or Cy5-UTP on templates isolated by RT-PCR from mouse Min6 cells (Ins2) or PCR from cloned XBP1 cDNA. The resulting products are gel purified to obtain full-length substrate. Reactions are then separated by 15% UREA-PAGE for analysis by phosphorimaging or by near-infrared imaging using the LI-COR Odyssey scanner.
細胞アッセイ 細胞株 Wild-type MEFs
濃度 ~128 μM
反応時間 24 hours
実験の流れ

Cells are seeded in phenol red-free cell culture medium in 96 or 24 well dishes at a density of 5 × 103 or 5 × 104 cells per well, respectively. Cultures are incubated for 16 h before treatment with 4μ8C for 24 h. Cultures are then analyzed by the addition of 200 μM WST1 and 10 μM phenazine metho-sulfate. After development of the reagent for 2 h at 37°C, the hydrolyzed dye is detected by absorbance at 450 nm, after subtracting background and absorbance at 595 nm. Alternatively, cell viability is determined by staining of the adherent culture with crystal violet. Quantitation of the dye uptake is analyzed by extensive washing of the stained cells with water and solublization of the crystal violet in methanol followed by absorbance measurements at 595 nm.
動物実験 動物モデル C57BL/6 mice
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/22315414/
  • https://pubmed.ncbi.nlm.nih.gov/24100031/
  • https://pubmed.ncbi.nlm.nih.gov/28137856/

カスタマーフィードバック

Data from [Data independently produced by , , Free Radic Biol Med, 2018, 124:395-407]

Data from [Data independently produced by , , Front Microbiol, 2017, 8:2129]

Data from [Data independently produced by , , Front Cell Infect Microbiol, 2017, 7:422]

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：

TaIRE1-mediated unconventional splicing of the TabZIP60 mRNA and the miR172 precursor regulates heat stress tolerance in wheat [ J Integr Plant Biol, 2025, 67(9):2388-2400.] PubMed: 40607649
TaIRE1-mediated unconventional splicing of the TabZIP60 mRNA and the miR172 precursor regulates heat stress tolerance in wheat [ J Integr Plant Biol, 2025, 10.1111/jipb.13963] PubMed: 40607649
The IRE1α/XBP1-mediated upregulation of LMTK2 attenuates endoplasmic reticulum stress by enhancing autophagic activity [ Cancer Lett, 2025, 633:217993] PubMed: 40834986
Curcumin Attenuates Fumonisin B1-Induced PK-15 Cell Apoptosis by Upregulating miR-1249 Expression to Inhibit the IRE1/MKK7/JNK/CASPASE3 Signaling Pathway [ Antioxidants (Basel), 2025, 14(2)168] PubMed: 40002355
Mitochondrial ROS-ER Stress Axis Governs IL-10 Production in Neutrophils and Regulates Inflammation in Murine Chlamydia pneumoniae Lung Infection [ Cells, 2025, 14(19)1523] PubMed: 41090752
Oridonin alleviates SiNPs-induced pulmonary fibrosis by inhibiting pyroptosis via IRE1α-XBP1s-NLRP3 pathway [ Int Immunopharmacol, 2025, 164:115388] PubMed: 40845545
PERK Regulates Epithelial-Mesenchymal Transition Through Autophagy and Lipid Metabolism in Lens Epithelial Cells [ Invest Ophthalmol Vis Sci, 2025, 66(5):35] PubMed: 40408092
TMED4 facilitates regulatory T cell suppressive function via ROS homeostasis in tumor and autoimmune mouse models [ J Clin Invest, 2024, 135(1)e179874] PubMed: 39480507
MANF facilitates breast cancer cell survival under glucose-starvation conditions via PRKN-mediated mitophagy regulation [ Autophagy, 2024, 1-22.] PubMed: 39147386
HSP47 Increases the Expression of Type I Collagen in Fibroblasts through IRE1α Activation, XBP1 Splicing, and Nuclear Translocation of β-Catenin [ Cells, 2024, 13(6)527] PubMed: 38534372

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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