For research use only.
CAS No. 14003-96-4
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.
Selleck's 4μ8C has been cited by 15 publications
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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.
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Choose Selective IRE1 Inhibitors
|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.|
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.  4μ8C, as an IRE1 inhibitor, blocks IL-4, IL-5, and IL-13 production from CD4+ T cells. 
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.
|In vitro||DMSO||19 mg/mL (93.05 mM)|
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