4μ8C

Name: 4μ8C
Brand: Selleck Chemicals
SKU: S7272
Rating: 5 (15 reviews)

For research use only.

Catalog No.S7272

15 publications

CAS No. 14003-96-4

4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

Selleck's 4μ8C has been cited by 15 publications

Cancer Lett, 2020, 28;476:67-74

PubMed: 32061752 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 8:269

PubMed: 32500072 ( click the link to review the publication )

Oncol Rep, 2020, 43(4):1245-1255

PubMed: 32323831 ( click the link to review the publication )

Cell Death Dis, 2019, 10(12):891

PubMed: 31767828 ( click the link to review the publication )

J Biol Chem, 2019, 294(9):3137-3151

PubMed: 30610118 ( click the link to review the publication )

Am J Transl Res, 2019, 11(2):641-654

PubMed: 30899368 ( click the link to review the publication )

Int J Biochem Cell Biol, 2019, 114:105572

PubMed: 31326465 ( click the link to review the publication )

Free Radic Biol Med, 2018, 124:395-407

PubMed: 29969718 ( click the link to review the publication )

J Cell Sci, 2018,

PubMed: 30131440 ( click the link to review the publication )

Sci Rep, 2018, 8(1):3496

PubMed: 29472690 ( click the link to review the publication )

Oncol Lett, 2018, 16(4):4729-4736

PubMed: 30214606 ( click the link to review the publication )

Parasit Vectors, 2018, 11(1):251

PubMed: 29665822 ( click the link to review the publication )

Front Microbiol, 2017, 8:2129

PubMed: 29163417 ( click the link to review the publication )

Front Cell Infect Microbiol, 2017, 7:422

PubMed: 29021973 ( click the link to review the publication )

Biochem Biophys Res Commun, 2017, 493(1):346-351.

PubMed: 28888981 ( click the link to review the publication )

5 Customer Reviews

H Representative immunofluorescence staining of TUNEL. Scale bars, 100 µm. I Representative images of DHE staining. Scale bars, 100 µm. Data are mean ± SEM, *p < 0.05, **p < 0.01, ***p < 0.001 by unpaired Student's t-test.

Free Radic Biol Med, 2018, 124:395-407. 4μ8C purchased from Selleck.
PK-15 cells were pretreated with 4μ8c (0, 1, 5, and 10 μM) for 6 h then infected with CSFV containing the corresponding concentrations of 4μ8c. After 24 h post infection, samples were collected and viral titers and copies were detected as described above. The inhibiting effect of 4μ8C on the IRE1-XBP1 signal was analyzed by detecting the splicing level of XBP1 and the expression of GRP78. Error bars represent the mean ± SD of 2 independent experiments; one-way ANOVA test; ∗P < 0.05, ∗∗P < 0.01.

Front Microbiol, 2017, 8:2129. 4μ8C purchased from Selleck.
Determination of LDH release. RAW264.7 cells both with and without 4μ8c (IRE1α inhibitor, 100 μM) treatment were infected with either S2308 or the ΔrfbE mutant at an MOI of 100. The supernatants were collected at 3, 5, and 8 hpi, and LDH release was detected using the CytoTox 96 nonradioactive cytotoxicity assay. The supernatants of uninfected RAW264.7 cells were used as negative controls (medium). ns, no significant difference, ***p < 0.0001.

Front Cell Infect Microbiol, 2017, 7:422. 4μ8C purchased from Selleck.
Role of the IRE1 pathway in the low-expression of adiponectin induced by hypoxia treatment in differentiated 3T3-L1 adipocytes. A. The gene expression of XBP1-s and XBP1-u at the mRNA level in differentiated 3T3-L1 adipocytes with the 4μ8C pretreatment for 2 h and hypoxia treatment for 12 h. B. Western blot analysis of XBP1-s and XBP1-u in adipocytes with the same treatment conditions as in A. C. The gene expression of adiponectin at mRNA levels in differentiated 3T3-L1 adipocytes with the same treatment conditions as in A. D. Western blot analysis of adiponectin with the same treatment conditions in A. The data shown represent the means ± S.E. values of 3–4 independent experiments. **p < 0.01 vs. normoxia; ***p < 0.001 vs. normoxia; ##p < 0.01 vs. hypoxia; ###p < 0.001 vs. hypoxia.

Biochem Biophys Res Commun, 2017, 493(1):346-351. 4μ8C purchased from Selleck.
IL-6 concentrations in cell-cultured mediums of IRE1α-overexpressing or XBP1s-overexpressing Hep3B cells with or without the presence of 4µ8C. Results are from at least three independent experiments. Data are presented as the mean ± standard error of the mean. *P<0.05, **P<0.01 by two-tailed unpaired Student's t-test or two-way analysis of variance. IRE1α, inositol-requiring enzyme 1α; XBP1, X-box-binding protein 1; IL-6, interleukin-6;

Oncol Lett, 2018, 16(4):4729-4736. 4μ8C purchased from Selleck.

Purity & Quality Control

Choose Selective IRE1 Inhibitors

Biological Activity

Description

4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.

Features

IRE1 Rnase-selective inhibitor, used as a platform for developing new locally acting drugs.

Targets

IRE1 Rnase ^[1]
(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 measureable acute toxicity. ^[1] 4μ8C, as an IRE1 inhibitor, blocks IL-4, IL-5, and IL-13 production from CD4+ T cells. ^[2]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
SF21 cells	NF\nWHRHfW6ldHnvckBie3OjeR?=	NFnvSWI{OCCvaX7z	NUn0UZJCUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDweZJqfGmwLVjpd{11[WepZXSgTXJGNTFiUl7hd4Uh\XiycnXzd4VlKGmwIGPGNlEh[2WubIOgeZNqdmdiWFLQMVEhWk6DIIP0[Y0hdG:xcDDhd{B{fWK\|dILheIUhcW6ldXLheIVlKG[xcjCzNEBucW6\|IIDybY9zKHSxIIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB{IHjyd{BjgSCIUlXUMZN2eHC{ZYPzbY9vKGG\|c3H5MEBKSzVyPUCuNlA3KM7:TR?=	NHzleIMzPDd2OUi2NS=>
human Jeko cells	NVHLfmZ4TnWwY4Tpc44h[XO\|YYm=	NFfmVGozPCCq	MoTWTY5pcWKrdHnvckBw\iC[QmCtNZMh\XiycnXzd4lwdiCrbjDoeY1idiCMZXvvJINmdGy\|IHHmeIVzKDJ2IHjyd{BjgSCrbX31co9jdG:2dHnu[{BidmGueYPpd{whUUN3ME2xMlU4KM7:TR?=	MX2yOFc1QTh4MR?=
human Mino cells	MYjGeY5kfGmxbjDhd5NigQ>?	MWOyOEBp	MXfJcohq[mm2aX;uJI9nKFiEUD2xd{BmgHC{ZYPzbY9vKGmwIHj1cYFvKE2rbn:gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGmvbYXuc4Jtd3S2aX7nJIFv[Wy7c3nzMEBKSzVyPUGuOlIh\|ryP	NXLQ[nRKOjR5NEm4OlE>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

^[1]

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In Vitro IRE1 RNase and RIDD Assays:

Analysis of radiolabeled Xbp1 substrate cleavage is performed as previously except that mammalian IRE1 reaction buffer is used. In vitro RIDD substrates are synthesized 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.

Cell Research:

^[1]

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Cell lines: Wild-type MEFs
Concentrations: ~128 μM
Incubation Time: 24 hours
Method:
Cells are seeded in phenol red-free cell culture medium in 96 or 24 well dishes at a density of 5 × 10³ or 5 × 10⁴ cells per well, respectively. Cultures are incubated for 16 h before treatment with 4μ8C for 24 h. Cultures are then analyzed by the addition of 200 μM WST1 and 10 μM phenazine metho-sulfate. After development of the reagent for 2 h at 37°C, the hydrolyzed dye is detected by absorbance at 450 nm, after subtracting background and absorbance at 595 nm. Alternatively, cell viability is determined by staining of the adherent culture with crystal violet. Quantitation of the dye uptake is analyzed by extensive washing of the stained cells with water and solublization of the crystal violet in methanol followed by absorbance measurements at 595 nm.

(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	19 mg/mL (93.05 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+40%PEG300+5%Tween80+50%ddH2O For best results, use promptly after mixing.	0.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download 4μ8C SDF

Molecular Weight	204.18
Formula	C₁₁H₈O₄
CAS No.	14003-96-4
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=CC(=O)OC2=C1C=CC(=C2C=O)O

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

ul

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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4μ8C