Name: Costunolide
Brand: Selleck Chemicals
SKU: S1319
Availability: InStock
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other Telomerase Inhibitors	EGCG ((-)-Epigallocatechin Gallate) BIBR 1532 RHPS 4 methosulfate Cycloastragenol TAC (TERT Activator-1) Cyclogalegenol Braco-19 trihydrochloride L-778123 hydrochloride Epitalon MST-312

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (202.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 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.
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.	2.000mg/ml (8.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 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.	1.400mg/ml (6.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 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.
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.

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	232.32	Formula	C₁₅H₂₀O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	553-21-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 106404			Smiles	CC1=CCCC(=CC2C(CC1)C(=C)C(=O)O2)C

Mechanism of Action

Targets/IC₅₀/Ki	FPTase 20 μM Telomerase (MDA-MB-231) 65 μM Telomerase (MCF-7) 90 μM
In vitro	Costunolide inhibits the growth and telomerase activity of MCF-7 and MDA-MB-231 cells in a concentration- and time-dependent manner. This compound also inhibits the farnesylation process of human lamin-B by farnesyl–proteinttransferase (FPTase), in a dose dependent manner. Continuously treatment of this chemical for 48 hours will significantly decrease proliferation of human tumor cells (A549, SK-OV-3, SK-MEL-2, XF498 and HCT-1) in a dose-dependent manner. It induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release to the cytosol in HL-60 human leukemia cells. A recent study indicates that this compound shows significant antifungal activity, including Trichophyton mentagrophytes, T.simlii, T.rubrum, and so on.
Kinase Assay	Telomerase activity assay
Kinase Assay	The telomerase activity is measured by the TRAP assay using the TRAPez Telomerase Detection Kit, which includes primers of a 36-bp internal control (IC) for quantifying the amplification of telomerase activity within a linear range close to 2.5 logs. For RNase treatment, 10μL of extract are incubated with 1μg of RNase at 37 °C for 20 minutes. The products of the TRAP assay are resolved by electrophoresis in a nondenaturing12% PAGE in a buffer containing 0.5 × Tris–borate EDTA and detected by autoradiograph. For quantification of TRAP products, the dried gels are exposed to Fuji Imaging Plate at room temperature. Results are corrected for background, and a standard value of 100 is given to the untreated control cell signal. Signal intensities of this compound-treated cells are compared to the standard and are expressed as a fraction of the maximum value of 100.
In vivo	Costunolide inhibits angiogenic response by blocking the angiogenic factor signaling pathway. In a mouse corneal micropocket assay, this compound reduces VEGF-stimulated neovascularization in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16112418/ [2] https://pubmed.ncbi.nlm.nih.gov/11458455/ [3] https://pubmed.ncbi.nlm.nih.gov/11256490/ [4] https://pubmed.ncbi.nlm.nih.gov/22397713/ [5] https://pubmed.ncbi.nlm.nih.gov/12359360/

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Costunolide Telomerase inhibitor

Chemical Structure

Molecular Weight: 232.32