A natural NF-κB inhibitor
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Wedelolactone

Item No. 11796

Technical Information
Formal Name
1,8,9-trihydroxy-3-methoxy-6H-benzofuro[3,2-c][1]benzopyran-6-one
CAS Number
524-12-9
Synonyms
  • IKK Inhibitor II
Molecular Formula
C16H10O7
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mLEthanol: 20 mg/mL
λmax
253, 351 nm
SMILES
OC1=CC2=C(OC(C(C(O)=CC(OC)=C3)=C3O4)=C2C4=O)C=C1O
InChi Code
InChI=1S/C16H10O7/c1-21-6-2-10(19)14-12(3-6)23-16(20)13-7-4-8(17)9(18)5-11(7)22-15(13)14/h2-5,17-19H,1H3
InChi Key
XQDCKJKKMFWXGB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Wedelolactone is a natural coumestan originally isolated from plants used in herbal therapies. It inhibits NF-κB signaling at the level of IKK action, resulting in suppression of NF-κB-mediated gene expression at concentrations of 1-100 µM.1,2,3 Wedelolactone can also inhibit hepatitis C virus NS5B RNA-dependent RNA polymerase in vitro (IC50 = 36 µM), STAT1 dephosphorylation (50 µM), and EZH2-EED interactions (Kd = 2.8 µM).4,5,6 Prolonged incubation of HepG2 liver cells with wedelolactone alters lipid metabolism through increased expression of AMPK, PPARα, lipoprotein lipase, and low-density lipoprotein receptor.7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kobori, M., Yang, Z., Gong, D., et alWedelolactone suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK complex. Cell Death Differ. 11(1), 123-130 (2004).

    2. Yuan, F., Chen, J., Sun, P.p., et alWedelolactone inhibits LPS-induced pro-inflammation via NF-kappaB pathway in RAW 264.7 cells. J. Biomed. Sci. 20:84, (2013).

    3. Alquézar, C., de la Encarnación, A., Moreno, F., et alProgranulin deficiency induces overactivation of WNT5A expression via TNF-α/NF-κB pathway in peripheral cells from frontotemporal dementia-linked granulin mutation carriers. J.Psychiatry Neurosci. 41(1), (2016).

    4. Kaushik-Basu, N., Bopda-Waffo, A., Talele, T.T., et alIdentification and characterization of coumestans as novel HCV NS5B polymerase inhibitors. Nucleic Acids Res. 35(5), 1482-1496 (2008).

    5. Chen, Z., Sun, X., Shen, S., et alWedelolactone, a naturally occurring coumestan, enhances interferon-γ signaling through inhibiting STAT1 protein dephosphorylation. The Journal of Biological Chemisty 288(20), 14417-14427 (2013).

    6. Chen, H., Gao, S., Li, J., et alWedelolactone disrupts the interaction of EZH2-EED complex and inhibits PRC2-dependent cancer. Oncotarget 6(15), 13049-13059 (2015).

    7. Zhao, Y., Peng, L., Yang, L.c., et alWedelolactone regulates lipid metabolism and improves hepatic steatosis partly by AMPK activation and up-regulation of expression of PPARa/LPL and LDLR. PLoS One 10(7), (2015).