Dehydrocostus Lactone

For research use only.

Catalog No.S3615

2 publications

Dehydrocostus Lactone Chemical Structure

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.

Size Price Stock Quantity  
USD 170 In stock
USD 447 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

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

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].

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].

Protocol

Cell Research:[2]
- Collapse
  • 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.
    (Only for Reference)
Animal Research:[2]
- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (199.73 mM)
Ethanol 46 mg/mL (199.73 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 230.30
Formula

C15H18O2

CAS No. 477-43-0
Storage powder
in solvent
Synonyms N/A
Smiles C=C1CCC2C(OC(=O)C2=C)C3C1CCC3=C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

IκB/IKK Signaling Pathway Map

Related IκB/IKK Products

Tags: buy Dehydrocostus Lactone | Dehydrocostus Lactone supplier | purchase Dehydrocostus Lactone | Dehydrocostus Lactone cost | Dehydrocostus Lactone manufacturer | order Dehydrocostus Lactone | Dehydrocostus Lactone distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID