Molecular Weight(MW): 230.30
Dehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.
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|Description||Dehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.|
Dehydrocostus lactone can inhibit PGE2 synthesis in vitro. It significantly decreases the expression of COX-2, but not that of COX-1. After treatment with DHE, the glioblastoma (U118, U251 or U87) cells are significantly inhibited in their viability, proliferation and migration. At the meantime, DHE also induces mitochondria-mediated apoptosis by promoting the release of cytochrome c into cytosol, which activating caspase signaling pathway. DHE significantly suppresses COX-2 expression by inhibiting the phosphorylation of IKKβ via targeting the ATP-binding site, thereby abrogating NF-κB binding and p300 recruitment to COX-2 promoter. DHE suppresses clonogenic and migratory ability of glioblastoma cells and induces apoptosis through mitochondrial pathway.
|In vivo||Dehydrocostus lactone suppresses the growth of colorecral cancer xenografts transplanted by colon cancer cell line colo205 in athymic mice. The inhibition effect is dose dependent. DHE can cross blood-brain barrier (BBB). Treatment with DHE markedly inhibits neoplastic weight and volume without the notable adverse effects in the xenograft nude mice model, and these effects may be mediated through inhibition of the IKKβ/NF-κB/COX-2 signaling pathway.|
|In vitro||DMSO||46 mg/mL (199.73 mM)|
|Ethanol||46 mg/mL (199.73 mM)|
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03874832||Completed||Drug: Dihydroergotamine||Migraine With Aura|Migraine Without Aura|Migraine||Satsuma Pharmaceuticals Inc.||September 11 2018||Phase 1|
|NCT03451162||Active not recruiting||Drug: DHES0815A||Breast Cancer||Genentech Inc.||April 17 2018||Phase 1|
|NCT01468558||Completed||Drug: MAP0004|Drug: IV DHE|Drug: Ketoconazole||Healthy||Allergan|MAP Pharmaceuticals Inc. a wholly owned subsidiary of Allergan||July 2010||Phase 1|
|NCT02862886||Completed||Other: myometrium biopsy||Pregnancy||Centre Hospitalier Universitaire Dijon||July 2010||Not Applicable|
|NCT01199965||Completed||Drug: MAP0004|Drug: IV DHE||Healthy Subjects||Allergan|MAP Pharmaceuticals Inc. a wholly owned subsidiary of Allergan||January 2010||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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