4μ8C (Synonyms: IRE1 Inhibitor III)

Name: 4μ8C
Brand: MedChemExpress
SKU: HY-19707
Rating: 5.0 (44 reviews)

Cat. No.: HY-19707 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

4μ8C Chemical Structure

CAS No. : 14003-96-4

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10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
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25 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
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Based on 44 publication(s) in Google Scholar

42 Publications Citing Use of MCE 4μ8C

: 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.

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Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
JeKo-1	IC₅₀	1.57 μM Compound: 5, 4mu8C	Inhibition of XBP-1s expression in human Jeko cells after 24 hrs by immunoblotting analysis Inhibition of XBP-1s expression in human Jeko cells after 24 hrs by immunoblotting analysis	[PMID: 24749861]
Sf21	IC₅₀	206 nM Compound: 5, 4mu8C	Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay Inhibition of human recombinant puritin-His-tagged IRE-1 RNase expressed in SF21 cells using XBP-1 RNA stem loop as substrate incubated for 30 mins prior to substrate addition measured after 2 hrs by FRET-suppression assay	[PMID: 24749861]

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.

14003-96-4

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
10 mM	0.4898 mL	2.4488 mL	4.8976 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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (122.44 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) HNMR (232 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Cross BC, et al. The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule. Proc Natl Acad Sci U S A. 2012 Apr 10;109(15):E869-78. [Content Brief]

[2]. Zhang L, et al. IRE1 inhibition perturbs the unfolded protein response in a pancreatic β-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis. BMC Cell Biol. 2014 Jul 10;15:29. [Content Brief]

[3]. Kemp K, et al. The serine-threonine kinase inositol-requiring enzyme 1α (IRE1α) promotes IL-4 production in T helper cells. J Biol Chem. 2013 Nov 15;288(46):33272-82.

[4]. Tufanli O, et al. Targeting IRE1 with small molecules counteracts progression of atherosclerosis. Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):E1395-E1404. [Content Brief]

[5]. Nam ST, et al. Suppression of IgE-mediated mast cell activation and mouse anaphylaxis via inhibition of Sykactivation by 8-formyl-7-hydroxy-4-methylcoumarin, 4μ8C. Toxicol Appl Pharmacol. 2017 Oct 1;332:25-31. [Content Brief]

Complete Stock Solution Preparation Table

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

4μ8C Related Classifications

Metabolic Disease

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.

Keywords:

4μ8C14003-96-4IRE1 Inhibitor IIIIRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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4μ8C (Synonyms: IRE1 Inhibitor III)

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4μ8C Related Antibodies

42 Publications Citing Use of MCE 4μ8C

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