4μ8C

製品コードS7272 バッチS727202

化学情報

	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	40 mg/mL (195.9 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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
キナーゼアッセイ	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

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：

A RIPK3-independent role of MLKL in suppressing parthanatos promotes immune evasion in hepatocellular carcinoma [ Cell Discov, 2023, 9(1):7]	PubMed: 36650126
ER stress induces caspase-2-tBID-GSDME-dependent cell death in neurons lytically infected with herpes simplex virus type 2 [ EMBO J, 2023, e113118.]	PubMed: 37646198
HRS mediates tumor immune evasion by regulating proteostasis-associated interferon pathway activation [ Cell Rep, 2023, 10.1016/j.celrep.2023.113352]	PubMed: 37948180
Carbonic anhydrase IX inhibitor S4 triggers release of DAMPs related to immunogenic cell death in glioma cells via endoplasmic reticulum stress pathway [ Cell Commun Signal, 2023, 21(1):167]	PubMed: 37386564
IRE1α arm of unfolded protein response in muscle-specific TGF-β signaling-mediated regulation of muscle cell immunological properties [ Cell Mol Biol Lett, 2023, 28(1):15]	PubMed: 36849929
Acute Endoplasmic Reticulum Stress Suppresses Hepatic Gluconeogenesis by Stimulating MAPK Phosphatase 3 Degradation [ Int J Mol Sci, 2023, 24(21)15561]	PubMed: 37958545
Large HBV Surface Protein-Induced Unfolded Protein Response Dynamically Regulates p27 Degradation in Hepatocellular Carcinoma Progression [ Int J Mol Sci, 2023, 10.3390/ijms241813825]	PubMed: 37762128
Seneca Valley Virus Degrades STING via PERK and ATF6-Mediated Reticulophagy [ Viruses, 2023, 10.3390/v15112209]	PubMed: 38005886
IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Pulm Pharmacol Ther, 2023, 10.1016/j.pupt.2023.102263]	PubMed: 37935327
Unconventional Activation of IRE1 Enhances TH17 Responses and Promotes Neutrophilic Airway Inflammation [ bioRxiv, 2023, 2023.06.30.547286]	PubMed: 37461622

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。