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

Purity & Quality Control

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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.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: 8-week-old C57BL/6J mice
  • Dosages: 0.5 mg/mouse
  • Administration: IP
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 94 mg/mL
(199.74 mM)
Ethanol 4 mg/mL
(8.49 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 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

In vivo Formulation Calculator (Clear solution)

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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.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04900025 Not yet recruiting Other: Bright lighting|Other: Placebo lighting Daytime Cognitive Performance|Sleep|Alertness University of Wisconsin Madison June 2024 Not Applicable
NCT04493229 Withdrawn Drug: Oxytocin|Drug: Placebo Osteoarthritis Knee Wake Forest University Health Sciences January 2024 Phase 2
NCT03813095 Not yet recruiting Drug: APH-1501|Drug: Placebo Addiction|Opioid Dependence|Opioid Withdrawal Aphios October 2023 Phase 2
NCT04565457 Not yet recruiting Device: Research CBCT Prostate Cancer|Head and Neck Cancers|Upper Abdomen Cancers University of Colorado Denver|National Cancer Institute (NCI) December 1 2022 Early Phase 1
NCT04100720 Not yet recruiting Device: Cardiovalve Transfemoral Tricuspid Valve Tricuspid Regurgitation Boston Biomedical Associates|Cardiovalve Ltd.|Cardiovascular Research Foundation New York October 2022 Not Applicable

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

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