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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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W424498-1ml | 1ml | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $241.90 |
Selective and irreversible IκB kinase inhibitor
Synonyms | Wedelolactone | 524-12-9 | 7-Methoxy-5,11,12-trihydroxycoumestan | 7-Methoxy-5,11,12-trihydroxy-coumestan | IKK Inhibitor II | 1,8,9-Trihydroxy-3-methoxycoumestan | CHEMBL97453 | 0K6L725GNS | CHEBI:10037 | 1,8,9-Trihydroxy-3-methoxy-6H-benzofuro[3,2-c]chromen-6-one | 5,11,12 |
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Specifications & Purity | Moligand™, 10mM in DMSO |
Biochemical and Physiological Mechanisms | Wedelolactone inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα. Irreversible inhibitor of IKKα and β kinase activity (IC50 < 10 μM). Wedelolactone has no effects on p38 MAP kinase or Akt.Selective |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies suggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies suggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin, and galactosamine, and inhibit 5-lipoxygenase (5-LO)) activity in porcine leukocytes. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 1,8,9-trihydroxy-3-methoxy-[1]benzofuro[3,2-c]chromen-6-one |
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INCHI | 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 |
Canonical SMILES | COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O |
Isomeric SMILES | COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O |
WGK Germany | 3 |
PubChem CID | 5281813 |
Molecular Weight | 314.25 |
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Sensitivity | Heat Sensitive |
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Melt Point(°C) | 315 °C |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed H317:May cause an allergic skin reaction |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P272:Contaminated work clothing should not be allowed out of the workplace. P333+P313:IF SKIN irritation or rash occurs: Get medical advice/attention. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
WGK Germany | 3 |
1. Du Si-Hao, Qiao Dong-Fang, Chen Chuan-Xiang, Chen Si, Liu Chao, Lin Zhoumeng, Wang Huijun, Xie Wei-Bing. (2017) Toll-Like Receptor 4 Mediates Methamphetamine-Induced Neuroinflammation through Caspase-11 Signaling Pathway in Astrocytes. Frontiers in Molecular Neuroscience, 10 (409). [PMID:29311802] [10.3389/fnmol.2017.00409] |
1. Du Si-Hao, Qiao Dong-Fang, Chen Chuan-Xiang, Chen Si, Liu Chao, Lin Zhoumeng, Wang Huijun, Xie Wei-Bing. (2017) Toll-Like Receptor 4 Mediates Methamphetamine-Induced Neuroinflammation through Caspase-11 Signaling Pathway in Astrocytes. Frontiers in Molecular Neuroscience, 10 (409). [PMID:29311802] [10.3389/fnmol.2017.00409] |