An IRE1α inhibitor
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4μ8C

Item No. 22110

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-hydroxy-4-methyl-2-oxo-2H-1-benzopyran-8-carboxaldehyde
CAS Number
14003-96-4
Synonyms
  • IRE1 Inhibitor III
Molecular Formula
C11H8O4
Formula Weight
204.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:8): 0.1 mg/mlDMSO: 25 mg/mlEthanol: 10 mg/ml
λmax
274 nm
SMILES
OC1=CC=C(C(C)=CC(O2)=O)C2=C1C=O
InChi Code
InChI=1S/C11H8O4/c1-6-4-10(14)15-11-7(6)2-3-9(13)8(11)5-12/h2-5,13H,1H3
InChi Key
RTHHSXOVIJWFQP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $41

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    10 mg

    $75

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    25 mg

    $128

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    50 mg

    $196

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    Cayman Chemical
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    Product Description

    4µ8C is an inhibitor of inositol requiring enzyme 1 α (IRE1α), which is a protein located in the endoplasmic reticulum (ER) membrane that has kinase and RNase activities triggered by ER stress.1 4µ8C inhibits IRE1α splicing of Xbp1 mRNA (IC50 = 6.8 µM) and reduces subsequent gene expression of Erdj4 (IC50 = 3.4 µM) in stress-cultured MEF cells but does not block IRE1α autophosphorylation. It reduces IL-4 production in CD4+ T cells isolated from murine spleen and LPS-stimulated increases in TNF-α and IL-6 mRNA expression and protein secretion in isolated alveolar macrophages from patients with cystic fibrosis.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cross, B.C., Bond, P.J., Sadowski, P.G., et al. The molecular basis for selective inhibition of unconventional mRNA splicing by an IRE1-binding small molecule. Proc. Natl. Acad. Sci. USA 109(15), E869-878 (2012).

    2. Kemp, K.L., Lin, Z., Zhao, F., et al. The serine-threonine kinase inositol-requiring enzyme 1α (IRE1α) promotes IL-4 production in T helper cells. The Journal of Biological Chemisty 288(46), 33272-33282 (2013).

    3. Lubamba, B.A., Jones, L.C., O'Neal, W.K., et al. X-box-binding protein 1 and innate immune responses of human cystic fibrosis alveolar macrophages. Am. J. Respir. Crit. Care Med. 192(12), 1449-1461 (2015).