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Submit ReviewArctigenin
Description: Potent MEK1 inhibitor. Also inhibits IκBα phosphorylation
Alternative Names: (-)-Arctigenin
Chemical Name: (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2(3H)-furanone
Purity: ≥98% (HPLC)
Biological Activity for Arctigenin
Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. Inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM). Inhibits HIV-1 replication in vitro. Also potently inhibits MKK1 (MEK1) (IC50 = 0.5 nM) and provides neuroprotection by binding to kainate receptors.
Compound Libraries for Arctigenin
Arctigenin is also offered as part of the Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Arctigenin
| M. Wt | 372.42 |
| Formula | C21H24O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 7770-78-7 |
| PubChem ID | 64981 |
| InChI Key | NQWVSMVXKMHKTF-JKSUJKDBSA-N |
| Smiles | OC(C=C3)=C(OC)C=C3C[C@@H](C(OC2)=O)[C@H]2CC1=CC(OC)=C(OC)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Arctigenin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.24 | 100 |
Preparing Stock Solutions for Arctigenin
The following data is based on the product molecular weight 372.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.69 mL | 13.43 mL | 26.85 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.37 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for Arctigenin
References for Arctigenin
References are publications that support the biological activity of the product.
Cho et al (2002) Potent inhibition of lipopolysaccharide-inducible nitric oxide synthase expression by dibenzylbutyrolactone lignans through inhibition of I-κBα phosphorylation and of p65 nuclear translocation. Int.Immunopharmacol. 2 105 PMID: 11789661
Jang et al (2002) Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor. J.Neurosci.Res. 68 233 PMID: 11948668
Schroder et al (1990) Differential in vitro anti-HIV activity of natural lignans. Z.Naturforsch.C. 45 1215 PMID: 1965681
Cho et al (2003) Arctigenin, a potent inhibitor of MKK1, inhibits lipopolysaccharide (LPS)-inducible nitric oxide synthase expression through inhibition of I-κBα phosphorylation and of p65 nuclear translocation. Exp.Biol.Abstr. 152.2
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Keywords: Arctigenin, Arctigenin supplier, inhibitors, IκB, IκBα, IkappaBalpha, phosphorylation, inhibits, MKK1, kainate, receptors, Nuclear, Factor, Kappa, B, Glutamate, Kainate, Receptors, iGluR, Ionotropic, Transcription, Factors, antiviral, NF-kB, NF-kappaB, NF-κB, (-)-Arctigenin, NF-kB/IkB, MEK, HIV, 1777, Tocris Bioscience
2 Citations for Arctigenin
Citations are publications that use Tocris products. Selected citations for Arctigenin include:
Rycaj et al (2016) Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells. Oncotarget 7 14220 PMID: 26871947
Ogungbe et al (2014) (-) Arctigenin and (+) pinoresinol are antagonists of the human thyroid hormone receptor β. J Chem Inf Model 54 3051 PMID: 25383984
Do you know of a great paper that uses Arctigenin from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for Arctigenin
