Name: 4μ8C
Brand: Selleck Chemicals
SKU: S7272
Rating: 5 (56 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	HSP JNK Antioxidant ROS eIF PERK PKR ASK PDI ATF-6
Other IRE1 Inhibitors	IXA4 Kira8 STF-083010 kira6 MKC-3946 MKC8866 APY29 6-Bromo-2-hydroxy-3-methoxybenzaldehyde

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
SF21 cells	Function assay	30 mins	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, IC50=0.206 μM
human Jeko cells	Function assay	24 h	Inhibition of XBP-1s expression in human Jeko cells after 24 hrs by immunoblotting analysis, IC50=1.57 μM
human Mino cells	Function assay	24 h	Inhibition of XBP-1s expression in human Mino cells after 24 hrs by immunoblotting analysis, IC50=1.62 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	204.18	Formula	C₁₁H₈O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	14003-96-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	IRE1 Inhibitor III			Smiles	CC1=CC(=O)OC2=C1C=CC(=C2C=O)O

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (347.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (2.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (4.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	IRE1 Rnase-selective inhibitor, used as a platform for developing new locally acting drugs.
Targets/IC₅₀/Ki	IRE1 Rnase (Cell-free assay) 76 nM
In vitro	4μ8C blocks substrate (RIDD) access to the active site of IRE1 and selectively inactivates both Xbp1 splicing and IRE1-mediated mRNA degradation. IRE1 inhibition subsequently induces ER stress without measurable acute toxicity. 4μ8C, as an IRE1 inhibitor, blocks IL-4, IL-5, and IL-13 production from CD4+ T cells.
Kinase Assay	In Vitro IRE1 RNase and RIDD Assays
Kinase Assay	Analysis of radiolabelled Xbp1 substrate cleavage is performed as previously except that mammalian IRE1 reaction buffer is used. In vitro RIDD substrates are synthesised 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. The resulting products are gel purified to obtain full-length substrate. Reactions are then separated by 15% UREA-PAGE for analysis by phosphorimaging or by near-infrared imaging using the LI-COR Odyssey scanner.
In vivo	4μ8c is an IRE1 Inhibitor III that reduces atherosclerotic lesion and effectively mitigates plaque development in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22315414/ [2] https://pubmed.ncbi.nlm.nih.gov/24100031/ [3] https://pubmed.ncbi.nlm.nih.gov/28137856/

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Handling Instructions

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4μ8C IRE1 inhibitor

Chemical Structure

Molecular Weight: 204.18