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

4μ8C (Synonyms: IRE1 Inhibitor III)

Cat. No.: HY-19707 Purity: 99.72%
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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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    4μ8C purchased from MCE. Usage Cited in: Toxins (Basel). 2020 Jan 16;12(1). pii: E55.

    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.
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    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].

    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].

    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.

    14003-96-4

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 27 mg/mL (132.24 mM)

    *"≥" 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
    10 mM 0.4898 mL 2.4488 mL 4.8976 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.72%

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    Keywords:

    4μ8CIRE1 Inhibitor IIIIRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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    Product Name:
    4μ8C
    Cat. No.:
    HY-19707
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