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

4μ8C (Synonyms: IRE1 Inhibitor III)

Cat. No.: HY-19707 Purity: 98.95%
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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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 70 In-stock
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25 mg USD 120 In-stock
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50 mg USD 190 In-stock
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100 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

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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
  4°C 2 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.
References
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4μ8C
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HY-19707
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