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Purity: ≥98%
4μ8C (also known as IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor (IC50 = 76 nM) with the potential for metabolic diseases. In addition to inhibiting Xbp1 splicing and IRE1-mediated mRNA degradation, 4μ8C also prevents substrate(RIDD) access to the active site of IRE1. Without detectable acute toxicity, IRE1 inhibition subsequently causes ER stress. 4μ8C, an IRE1 inhibitor, prevents CD4+ T cells from producing IL-4, IL-5, and IL-13.
| Targets |
IRE1 Rnase (IC50 = 76 nM)
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| ln Vitro |
In addition to inhibiting Xbp1 splicing and IRE1-mediated mRNA degradation, 4μ8C also prevents substrate(RIDD) access to the active site of IRE1. Without detectable acute toxicity, IRE1 inhibition subsequently causes ER stress.[1]
4μ8C, blocks CD4+ T cells' ability to produce IL-4, IL-5, and IL-13 by acting as an IRE1 inhibitor.[2]
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| ln Vivo |
4μ8c is an IRE1 Inhibitor III that decreases atherosclerotic lesions and effectively prevents plaque development in mice.
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| Enzyme Assay |
The same procedure as before is followed for the analysis of radiolabeled Xbp1 substrate cleavage, with the exception that mammalian IRE1 reaction buffer is employed. In vitro RIDD substrates are produced 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. To obtain full-length substrate, the produced products are gel purified. The reactions are next separated by 15% UREA-PAGE before being subjected to phosphorimaging or near-infrared imaging using the LI-COR Odyssey scanner for analysis.
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| Cell Assay |
In 96 or 24 well dishes, cells are seeded at a density of 5 × 103 or 5 × 104 per well in phenol red-free cell culture medium. Before being exposed to 48C for 24 hours, cultures are incubated for 16 hours. The addition of 200 M WST1 and 10 M phenazine metho-sulfate is then used to analyze the cultures. The hydrolyzed dye is detected by absorbance at 450 nm, after subtracting background and absorbance at 595 nm, following development of the reagent for 2 h at 37 °C. As an alternative, the adherent culture can be stained with crystal violet to determine the viability of the cells. After thoroughly washing the stained cells in water and dissolving the crystal violet in methanol, absorbance measurements at 595 nm are used to quantify the dye uptake.
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| Animal Protocol |
C57BL/6 mice
10 mg/kg i.p. |
| References |
| Molecular Formula |
C11H8O4
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|---|---|---|
| Molecular Weight |
204.18
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| Exact Mass |
204.04
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| Elemental Analysis |
C, 64.71; H, 3.95; O, 31.34
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| CAS # |
14003-96-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=CC(=O)OC2=C1C=CC(=C2C=O)O
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| InChi Key |
RTHHSXOVIJWFQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H8O4/c1-6-4-10(14)15-11-7(6)2-3-9(13)8(11)5-12/h2-5,13H,1H3
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| Chemical Name |
7-hydroxy-4-methyl-2-oxochromene-8-carbaldehyde
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 0.5mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8976 mL | 24.4882 mL | 48.9764 mL | |
| 5 mM | 0.9795 mL | 4.8976 mL | 9.7953 mL | |
| 10 mM | 0.4898 mL | 2.4488 mL | 4.8976 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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