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Withaferin A (WFA) NF-κB inhibitor

Name: Withaferin A (WFA)
Brand: Selleck Chemicals
SKU: S8587
Rating: 5 (13 reviews)

Cat.No.S8587

This steroidal lactone, isolated from Withania somnifera, potently inhibits NF-κB activation by preventing the tumour necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism. It also binds to the intermediate filament (IF) protein, vimentin, with antitumor and antiangiogenesis activity.

Chemical Structure

Molecular Weight: 470.60

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other NF-κB Inhibitors	DCZ0415 Omaveloxolone (RTA-408) BAY 11-7082 (BAY 11-7821) JSH-23 QNZ (EVP4593) Caffeic Acid Phenethyl Ester SC75741 DHA (Dihydroartemisinin) Andrographolide Evodiamine

Chemical Information, Storage & Stability

Molecular Weight	470.60	Formula	C₂₈H₃₈O₆	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	5119-48-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.	4.850mg/ml (10.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 97 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.	1.210mg/ml (2.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 24.2 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.

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB vimentin
In vitro	Withaferin A (WFA) potently inhibits NFκB activation by preventing the tumor necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism. It binds to the intermediate filament (IF) protein, vimentin, by covalently modifying its cysteine residue, which is present in the highly conserved α-helical coiled coil 2B domain, and induces vimentin filaments to aggregate in vitro.
In vivo	Withaferin A (WFA) clearly displays anti-inflammatory characteristics in an acute inflammatory mouse model. Its induced inhibition of capillary growth in a mouse model of corneal neovascularization is compromised in vimentin-deficient mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17150968/ [2] https://pubmed.ncbi.nlm.nih.gov/17584610/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01199250	Not yet recruiting	Lynch Syndrome\|Recurrent Uterine Corpus Carcinoma\|Stage I Uterine Corpus Cancer\|Stage II Uterine Corpus Cancer\|Stage III Uterine Corpus Cancer\|Stage IV Uterine Corpus Cancer	Gynecologic Oncology Group\|National Cancer Institute (NCI)\|GOG Foundation	January 2100	--
NCT04432610	Withdrawn	Nebivolol Adverse Reaction	Clinical Hospital Center Zemun	January 2030	Phase 4
NCT06376812	Not yet recruiting	Elevated Blood Pressure\|Perimenopause	The University of Texas Medical Branch Galveston	May 2026	Not Applicable

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