Withaferin A

Catalog No.S8587 Synonyms: WA, WFA

For research use only.

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

Withaferin A Chemical Structure

CAS No. 5119-48-2

Selleck's Withaferin A has been cited by 7 Publications

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Biological Activity

Description Withaferin A (WA, WFA) potently inhibits NF-κB activation by preventing the tumor necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism. Withaferin A binds to the intermediate filament (IF) protein, vimentin with antitumor and antiangiogenesis activity. Withaferin A is a steroidal lactone isolated from Withania somnifera.
Targets
NF-κB [1] vimentin [2]
In vitro

Withaferin A potently inhibits NFκB activation by preventing the tumor necrosis factor-induced activation of IκB kinase β via a thioalkylation-sensitive redox mechanism.[1] Withaferin A 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. Withaferin A induces vimentin filaments to aggregate in vitro.[2]

In vivo

Withagerin A clearly displays anti-inflammatory characteristics in an acute inflammatory mouse model.[1] Withagerin A-induced inhibition of capillary growth in a mouse model of corneal neovascularization is compromised in vimentin-deficient mice.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: HUVECs, BAECs,MCF-7 breast cancer cell line, MFT-16 cells
  • Concentrations: 5 μM, 10 μM
  • Incubation Time: 1 h, 2 h, 24 h
  • Method:

    To assess the apoptosis activity of WFA and 12-D WS, embryonic fibroblast vimentindeficient cell lines (Vim−/−; MFT-16) and wild-type (Vim+/+; MFT-6) cells are treated with 5 μM WFA, 5 μM 12-D WS, or an equivalent amount of vehicle (DMSO) for 24 hr in 37℃-5% CO2 conditions in complete medium. Apoptotic cells are measured with the Vybrant Apoptosis Assay Kit according to the manufacturer's instructions.

Animal Research:

[1]

  • Animal Models: 8-week-old C57BL/6J mice
  • Dosages: 0.5 mg/mouse
  • Administration: IP

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 470.60
Formula

C28H38O6

CAS No. 5119-48-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=O)OC(C1)C(C)C2CCC3C2(CCC4C3CC5C6(C4(C(=O)C=CC6O)C)O5)C)CO

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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.

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

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01199250 Not yet recruiting Other: Laboratory Biomarker Analysis 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 --
NCT05260801 Not yet recruiting Other: Bright Lighting|Other: Placebo Lighting Daytime Cognitive Performance|Sleep|Alertness Arizona State University December 1 2024 Not Applicable
NCT04774965 Not yet recruiting Device: Slumber Curve sleep aid Rotator Cuff Tears|Surgery|Pain Postoperative University of Alabama at Birmingham|Eight28 LLC June 30 2024 Not Applicable
NCT03806751 Not yet recruiting Drug: [O-15]Water|Drug: Acetazolamide Validation of a New Noninvasive Method to Obtain the Arterial Input Function (AIF) Directly by PET Imaging University of Alabama at Birmingham February 1 2024 Early Phase 1
NCT04493229 Withdrawn Drug: Oxytocin|Drug: Placebo Osteoarthritis Knee Wake Forest University Health Sciences January 2024 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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Handling Instructions

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