4μ8C

Catalog No.S7272

4μ8C Chemical Structure

Molecular Weight(MW): 204.18

4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

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USD 470 In stock
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Cited by 5 Publications

5 Customer Reviews

  • H Representative immunofluorescence staining of TUNEL. Scale bars, 100 µm. I Representative images of DHE staining. Scale bars, 100 µm. Data are mean ± SEM, *p < 0.05, **p < 0.01, ***p < 0.001 by unpaired Student's t-test.

    Free Radic Biol Med, 2018, 124:395-407. 4μ8C purchased from Selleck.

    PK-15 cells were pretreated with 4μ8c (0, 1, 5, and 10 μM) for 6 h then infected with CSFV containing the corresponding concentrations of 4μ8c. After 24 h post infection, samples were collected and viral titers and copies were detected as described above. The inhibiting effect of 4μ8C on the IRE1-XBP1 signal was analyzed by detecting the splicing level of XBP1 and the expression of GRP78. Error bars represent the mean ± SD of 2 independent experiments; one-way ANOVA test; ∗P < 0.05, ∗∗P < 0.01.

    Front Microbiol, 2017, 8:2129. 4μ8C purchased from Selleck.

  • Determination of LDH release. RAW264.7 cells both with and without 4μ8c (IRE1α inhibitor, 100 μM) treatment were infected with either S2308 or the ΔrfbE mutant at an MOI of 100. The supernatants were collected at 3, 5, and 8 hpi, and LDH release was detected using the CytoTox 96 nonradioactive cytotoxicity assay. The supernatants of uninfected RAW264.7 cells were used as negative controls (medium). ns, no significant difference, ***p < 0.0001.

    Front Cell Infect Microbiol, 2017, 7:422. 4μ8C purchased from Selleck.

    Role of the IRE1 pathway in the low-expression of adiponectin induced by hypoxia treatment in differentiated 3T3-L1 adipocytes. A. The gene expression of XBP1-s and XBP1-u at the mRNA level in differentiated 3T3-L1 adipocytes with the 4μ8C pretreatment for 2 h and hypoxia treatment for 12 h. B. Western blot analysis of XBP1-s and XBP1-u in adipocytes with the same treatment conditions as in A. C. The gene expression of adiponectin at mRNA levels in differentiated 3T3-L1 adipocytes with the same treatment conditions as in A. D. Western blot analysis of adiponectin with the same treatment conditions in A. The data shown represent the means ± S.E. values of 3–4 independent experiments. **p < 0.01 vs. normoxia; ***p < 0.001 vs. normoxia; ##p < 0.01 vs. hypoxia; ###p < 0.001 vs. hypoxia.

    Biochem Biophys Res Commun, 2017, 493(1):346-351. 4μ8C purchased from Selleck.

  • IL-6 concentrations in cell-cultured mediums of IRE1α-overexpressing or XBP1s-overexpressing Hep3B cells with or without the presence of 4µ8C. Results are from at least three independent experiments. Data are presented as the mean ± standard error of the mean. *P<0.05, **P<0.01 by two-tailed unpaired Student's t-test or two-way analysis of variance. IRE1α, inositol-requiring enzyme 1α; XBP1, X-box-binding protein 1; IL-6, interleukin-6;

    Oncol Lett, 2018, 16(4):4729-4736. 4μ8C purchased from Selleck.

Purity & Quality Control

Choose Selective IRE1 Inhibitors

Biological Activity

Description 4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Features IRE1 Rnase-selective inhibitor, used as a platform for developing new locally acting drugs.
Targets
IRE1 Rnase [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF21 cells NHrNZ|ZHfW6ldHnvckBie3OjeR?= MX[zNEBucW6| MoLITY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCydYLpeIlvNUircz30ZYdo\WRiSWLFMVEhWk6jc3Wg[ZhxemW|c3XkJIlvKFOIMkGgZ4VtdHNidYPpcochYEKSLUGgVm5CKHO2ZX2gcI9weCCjczDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiB|MDDtbY5{KHC{aX;yJJRwKHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAzKGi{czDifUBHWkWWLYP1dJBz\XO|aX;uJIF{e2G7LDDJR|UxRTBwMkC2JO69VQ>? M1zzb|I1PzR7OE[x
human Jeko cells NEn4UoxHfW6ldHnvckBie3OjeR?= MkP3NlQhcA>? MXTJcohq[mm2aX;uJI9nKFiEUD2xd{BmgHC{ZYPzbY9vKGmwIHj1cYFvKEqna3:gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGmvbYXuc4Jtd3S2aX7nJIFv[Wy7c3nzMEBKSzVyPUGuOVch|ryP NV\CTYh4OjR5NEm4OlE>
human Mino cells NYnDNXNKTnWwY4Tpc44h[XO|YYm= NGfIO3IzPCCq NHv5N21KdmirYnn0bY9vKG:oIGjCVE0yeyCneIDy[ZN{cW:wIHnuJIh2dWGwIF3pco8h[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvPjJizszN MYSyOFc1QTh4MR?=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[1]

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  • Cell lines: Wild-type MEFs
  • Concentrations: ~128 μM
  • Incubation Time: 24 hours
  • Method:

    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)

Solubility (25°C)

In vitro DMSO 19 mg/mL (93.05 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5%Tween 80+H2O
For best results, use promptly after mixing.
2mg/mL

* 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.

Chemical Information

Molecular Weight 204.18
Formula

C11H8O4

CAS No. 14003-96-4
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID