Home ER stress & UPR IRE1 inhibitor 4μ8C For research use only.

4μ8C

Synonyms: IRE1 Inhibitor III

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

4μ8C Chemical Structure

4μ8C Chemical Structure

CAS: 14003-96-4

Selleck's 4μ8C has been cited by 40 publications

Purity & Quality Control

Batch: Purity: 99.75%
99.75

4μ8C Related Products

Choose Selective IRE1 Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SF21 cells Function assay 30 mins Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay, IC50=0.206 μM 24749861
human Jeko cells Function assay 24 h Inhibition of XBP-1s expression in human Jeko cells after 24 hrs by immunoblotting analysis, IC50=1.57 μM 24749861
human Mino cells Function assay 24 h Inhibition of XBP-1s expression in human Mino cells after 24 hrs by immunoblotting analysis, IC50=1.62 μM 24749861
Click to View More Cell Line Experimental Data

Biological Activity

Description 4μ8C (IRE1 Inhibitor III) 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
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]
Kinase Assay 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 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.
In Vivo
In vivo

4μ8c is an IRE1 Inhibitor III that reduces atherosclerotic lesion and effectively mitigate plaque development in mice.
Animal Research Animal Models C57BL/6 mice
Dosages 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 204.18 Formula

C11H8O4
CAS No. 14003-96-4 SDF Download 4μ8C SDF
Smiles CC1=CC(=O)OC2=C1C=CC(=C2C=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (347.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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