1. Cell Cycle/DNA Damage
  2. IRE1
  3. 4μ8C

4μ8C  (Synonyms: IRE1 Inhibitor III)

Cat. No.: HY-19707 Purity: 98.78%
COA Handling Instructions

4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.

For research use only. We do not sell to patients.

4μ8C Chemical Structure

4μ8C Chemical Structure

CAS No. : 14003-96-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
25 mg USD 132 In-stock
50 mg USD 209 In-stock
100 mg USD 319 In-stock
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Customer Review

Based on 34 publication(s) in Google Scholar

Top Publications Citing Use of Products

32 Publications Citing Use of MCE 4μ8C

WB

    4μ8C purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2023 Apr 18.  [Abstract]

    4μ8C (20 μM; 1 h) significantly inhibits NaF-induced increased expression of p-IRE1 , GRP78 , p-TRAF2 , p-JNK, and LC3II/I in LS8 cells.

    4μ8C purchased from MedChemExpress. Usage Cited in: Toxins. 2020 Jan 16;12(1):55.  [Abstract]

    The effect of the IRE1 specific inhibitor 4μ8C on the expression of apoptosis-related proteins. The cells are exposed to FB1 with or without 4μ8C for 24 h, and the phosphorylation of JNK, Mcl-1, Bak, Bax, and Puma were analyzed by Western blotting. n = 3.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.

    In Vitro

    When applies to the media of ER stressed cultured cells, 4μ8C (IRE1 Inhibitor III) inhibits Xbp1 splicing in a concentration-dependent manner. 4μ8C dissociates slowly from IRE1, but ishout of inhibitor leads to rapid recovery of Xbp1 splicing in cells[1].The IRE1 endoribonuclease inhibitor 4μ8c prevents the splicing of the XBP1 mRNA in response to ER stress caused by mutant proinsulin production[2]. The inositol-requiring enzyme 1α (IRE1α) is a serine-threonine kinase that plays crucial roles in activating the unfolded protein response. 4μ8C treatment dramatically inhibits IL-4 production by CD4+ T cells under Th0 conditions because both the IL-4 levels in the culture supernatant and the percentage of IL-4 positive cells are reduced by 4μ8C treatment. In addition, both IL-5 and IL-13 production are significantly reduced upon treatment with 4μ8C[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    4μ8c (IRE1 Inhibitor III) (i.p. injection; 10 mg/kg/day for 4 more weeks) leads to a significant reduction (45.2%) in atherosclerotic lesion area in en face aorta preparations. 4μ8c can effectively mitigate plaque development in mice[4].
    ? 4μ8C (orally; 10, 50, or 100 mg/kg) suppresses passive cutaneous anaphylaxis (PCA) in mice (ED50 = 25.1 mg/kg)[5].
    ? 4μ8C reverses the ER stress-dependent loss of several known RIDD targets, with an EC50 of approximately 4 μM, approximating that of inhibition of XBP1 target gene activation[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: ApoE-/- mice[4]
    Dosage: 10 mg/kg
    Administration: I.p. injection; daily; for 4 more weeks
    Result: Led to a significant reduction (45.2%) in atherosclerotic lesion area in en face aorta preparations.
    Molecular Weight

    204.18

    Formula

    C11H8O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=CC1=C(O)C=CC2=C1OC(C=C2C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 27 mg/mL (132.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (10.19 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.78%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.8976 mL 24.4882 mL 48.9764 mL 122.4410 mL
    5 mM 0.9795 mL 4.8976 mL 9.7953 mL 24.4882 mL
    10 mM 0.4898 mL 2.4488 mL 4.8976 mL 12.2441 mL
    15 mM 0.3265 mL 1.6325 mL 3.2651 mL 8.1627 mL
    20 mM 0.2449 mL 1.2244 mL 2.4488 mL 6.1220 mL
    25 mM 0.1959 mL 0.9795 mL 1.9591 mL 4.8976 mL
    30 mM 0.1633 mL 0.8163 mL 1.6325 mL 4.0814 mL
    40 mM 0.1224 mL 0.6122 mL 1.2244 mL 3.0610 mL
    50 mM 0.0980 mL 0.4898 mL 0.9795 mL 2.4488 mL
    60 mM 0.0816 mL 0.4081 mL 0.8163 mL 2.0407 mL
    80 mM 0.0612 mL 0.3061 mL 0.6122 mL 1.5305 mL
    100 mM 0.0490 mL 0.2449 mL 0.4898 mL 1.2244 mL
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    4μ8C Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    4μ8C
    Cat. No.:
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