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Dehydrocostus Lactone IκB/IKK inhibitor

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

Cat.No.S3615

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.

Chemical Structure

Molecular Weight: 230.30

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	NF-κB HDAC Antioxidant ROS Nrf2 AP-1 MALT NOD
Other IκB/IKK Inhibitors	TBK1/IKKε-IN-5 Wedelolactone IKK-16 TPCA-1 Bay 11-7085 BMS-345541 IMD 0354 MRT67307 HCl SC-514 LY2409881

Solubility

In vitro
Batch:

DMSO : 46 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.3mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.32mg/ml (1.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	230.30	Formula	C₁₅H₁₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	477-43-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C=C1CCC2C(C3C1CCC3=C)OC(=O)C2=C

Mechanism of Action

Targets/IC₅₀/Ki	IKKβ COX2
In vitro	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.
References	[1] http://cancerres.aacrjournals.org/content/64/7_Supplement/230.1 [2] https://pubmed.ncbi.nlm.nih.gov/28670490/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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