Name: Dehydrocostus Lactone
Brand: Selleck Chemicals
SKU: S3615
Rating: 5 (3 reviews)

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 Chemical Structure

CAS: 477-43-0

Selleck's Dehydrocostus Lactone has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Dehydrocostus Lactone Related Products

Related Targets	IκB IKK	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Immunology/Inflammation Compound Library Small Molecule Immuno-Oncology Compound Library NF-κB Signaling Compound Library FDA-approved Anticancer Drug Library	Click to Expand

Signaling Pathway

IκB/IKK Signaling Pathway

Choose Selective IκB/IKK Inhibitors

Biological Activity

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.

Targets

IKKβ ^[2]

COX2 ^[1]

In vitro
In vitro	Dehydrocostus lactone can inhibit PGE2 synthesis in vitro. It significantly decreases the expression of COX-2, but not that of COX-1^[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^[2].
Cell Research	Cell lines	U118, U251 and U87 cells
	Concentrations	0, 1, 10, 25, 50 and 100 μM
	Incubation Time	12, 24, 36 or 48 h
	Method	U118 (6×10³ cells/well), U251 (8×10³ cells/well) and U87 (7×10³ cells/well) cells are counted and allowed to adhere to obtain 70% confluent monolayer. Following this, the cells are treated with different concentrations of DHE as indicated. After incubation for 12, 24, 36 or 48 h, 10 μl of MTT (5 mg/ml) is added to each well and the cells are incubated for another 4 h. Subsequently, the medium is replaced with 100 μl of DMSO to dissolve formazan crystals. The absorbance is measured at 570 nm using a microplate reader. Each experiment is repeated at least three times. The IC50 values are calculated by interpolation from dose-response curves.

In Vivo
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^[1]. 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^[2].
Animal Research	Animal Models	The female athymic nude mice (4-6 weeks old) and Sprague Dawley rats (8-10 weeks old)
	Dosages	10 and 20 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05337254	Completed	Migraine\|Migraine With Aura\|Migraine Without Aura	Satsuma Pharmaceuticals Inc.	March 5 2021	Phase 1
NCT03874832	Completed	Migraine With Aura\|Migraine Without Aura\|Migraine	Satsuma Pharmaceuticals Inc.	September 11 2018	Phase 1
NCT03451162	Completed	Breast Cancer	Genentech Inc.	April 17 2018	Phase 1
NCT01468558	Completed	Healthy	Allergan\|MAP Pharmaceuticals Inc. a wholly owned subsidiary of Allergan	July 2010	Phase 1
NCT02862886	Completed	Pregnancy	Centre Hospitalier Universitaire Dijon	July 2010	Not Applicable

References

Chemical Information & Solubility

Molecular Weight	230.30	Formula	C₁₅H₁₈O₂
CAS No.	477-43-0	SDF	Download Dehydrocostus Lactone SDF
Smiles	C=C1CCC2C(C3C1CCC3=C)OC(=O)C2=C
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 46 mg/mL ( (199.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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