4μ8C

Catalog No.S7272 Synonyms: IRE1 Inhibitor III

For research use only.

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

4μ8C Chemical Structure

CAS No. 14003-96-4

Selleck's 4μ8C has been cited by 24 publications

Purity & Quality Control

Choose Selective IRE1 Inhibitors

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

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 MlfpSpVv[3Srb36gZZN{[Xl? NXnCZZBlOzBibXnudy=> NWHhNYplUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDweZJqfGmwLVjpd{11[WepZXSgTXJGNTFiUl7hd4Uh\XiycnXzd4VlKGmwIGPGNlEh[2WubIOgeZNqdmdiWFLQMVEhWk6DIIP0[Y0hdG:xcDDhd{B{fWK|dILheIUhcW6ldXLheIVlKG[xcjCzNEBucW6|IIDybY9zKHSxIIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB{IHjyd{BjgSCIUlXUMZN2eHC{ZYPzbY9vKGG|c3H5MEBKSzVyPUCuNlA3KM7:TR?= M2fy[FI1PzR7OE[x
human Jeko cells MmHQSpVv[3Srb36gZZN{[Xl? MXGyOEBp NE[5Vm9KdmirYnn0bY9vKG:oIGjCVE0yeyCneIDy[ZN{cW:wIHnuJIh2dWGwIFrlb48h[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4T0bY5oKGGwYXz5d4l{NCCLQ{WwQVEvPTdizszN MmTNNlQ4PDl6NkG=
human Mino cells MoDlSpVv[3Srb36gZZN{[Xl? MX6yOEBp MnLITY5pcWKrdHnvckBw\iC[QmCtNZMh\XiycnXzd4lwdiCrbjDoeY1idiCPaX7vJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2dHnu[{BidmGueYPpd{whUUN3ME2xMlYzKM7:TR?= M3qwdVI1PzR7OE[x

Protocol (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.

0.5mg/mL

Chemical Information

Molecular Weight 204.18
Formula

C11H8O4

CAS No. 14003-96-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=O)OC2=C1C=CC(=C2C=O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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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