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4μ8C

4μ8C

产品编号 T6363   CAS 14003-96-4
别名: IRE1 Inhibitor III

4μ8C (IRE1 Inhibitor III) 是一种有效且特异性的 IRE1α 抑制剂。

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4μ8C Chemical Structure
4μ8C, CAS 14003-96-4
规格 价格/CNY 货期 数量
1 mg ¥ 218 现货
5 mg ¥ 497 现货
10 mg ¥ 822 现货
25 mg ¥ 1,570 现货
50 mg ¥ 2,390 现货
100 mg ¥ 3,570 现货
500 mg ¥ 7,880 现货
1 mL * 10 mM (in DMSO) ¥ 497 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: 4μ8C (T6363)
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纯度: 98.61%
纯度: 97.48%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
靶点活性 IRE1 Rnase:76 nM
体外活性 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]
体内活性 4μ8C reverses the ER stress-dependent loss of several known RIDD targets, with an EC50 of approximately 4 μM, approximating that of inhibition of XBP1 target gene activation[1].
激酶实验 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.
细胞实验 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. (Only for Reference)
别名 IRE1 Inhibitor III
分子量 204.18
分子式 C11H8O4
CAS No. 14003-96-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 20.4 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8976 mL 24.4882 mL 48.9764 mL 122.441 mL
5 mM 0.9795 mL 4.8976 mL 9.7953 mL 24.4882 mL
10 mM 0.4898 mL 2.4488 mL 4.8976 mL 12.2441 mL
20 mM 0.2449 mL 1.2244 mL 2.4488 mL 6.122 mL
50 mM 0.098 mL 0.4898 mL 0.9795 mL 2.4488 mL
100 mM 0.049 mL 0.2449 mL 0.4898 mL 1.2244 mL

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TargetMol Library Books参考文献

1. Cross BC, et al. Proc Natl Acad Sci U S A. 2012, 109(15), E869-878. 2. Kemp KL, et al. J Biol Chem. 2013, 288(46), 33272-33282.

TargetMol Library Books文献引用

1. Chen Y, Wu Z, Huang S, et al. Adipocyte IRE1α promotes PGC1α mRNA decay and restrains adaptive thermogenesis. Nature Metabolism. 2022: 1-19. 2. Cai J, Zhang X, Chen P, et al. The ER stress sensor inositol-requiring enzyme 1α in Kupffer cells promotes hepatic ischemia-reperfusion injury. Journal of Biological Chemistry. 2021: 101532. 3. Luo R, Wei Y, Chen P, et al.Mesenchymal Stem Cells Inhibit Epithelial-to-Mesenchymal Transition by Modulating the IRE1α Branch of the Endoplasmic Reticulum Stress Response.Stem Cells International.2023, 2023. 4. Gao K, Yi Y, Xue Z, et al.Downregulation of XBP1s aggravates lipopolysaccharide-induced inflammation by promoting NF-κB and NLRP3 pathways’ activation in goat endometrial epithelial cells.Theriogenology.2023
MKC8866 GSK2850163 B I09 IXA6 Sunitinib Malate APY29 Kira8 6-Bromo-2-hydroxy-3-methoxybenzaldehyde

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 高选择性抑制剂库 细胞周期化合物库 经典已知活性库 表型筛选靶点鉴定库 抗衰老化合物库 抗癌化合物库 NO PAINS 化合物库 已知活性化合物库 内质网应激化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

4μ8C 14003-96-4 Cell Cycle/Checkpoint IRE1 IRE1 Inhibitor III 4mu8C Inhibitor Inositol requiring enzyme 1 inhibit inhibitor

 

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