Withaferin A (WFA)

Catalog No.S8587 Batch:S858701

Technical Data

Formula	C₂₈H₃₈O₆
Molecular Weight	470.60	CAS No.	5119-48-2
Solubility (25°C)*	In vitro	DMSO	94 mg/mL (199.74 mM)
		Ethanol	4 mg/mL (8.49 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Withaferin A (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 Assay:^{^[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 Study:^{^[1]}	Animal Models 8-week-old C57BL/6J mice Dosages 0.5 mg/mouse Administration IP

Cell Assay:^{^[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 Study:^{^[1]}

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

References

Selleck's Withaferin A (WFA) has been cited by 10 publications

A Gene Co-Expression Network-Based Drug Repositioning Approach Identifies Candidates for Treatment of Hepatocellular Carcinoma [ Cancers (Basel), 2022, 14(6)1573]	PubMed: 35326724
A redox-sensitive iron-sulfur cluster in murine FAM72A controls its ability to degrade the nuclear form of uracil-DNA glycosylase [ DNA Repair (Amst), 2022, 118:103381]	PubMed: 35908367
HIV-1 Proteins gp120 and Tat Promote Epithelial-Mesenchymal Transition and Invasiveness of HPV-Positive and HPV-Negative Neoplastic Genital and Oral Epithelial Cells [ Microbiol Spectr, 2022, 10(6):e0362222.]	PubMed: 36314970
Withaferin A Triggers Apoptosis and DNA Damage in Bladder Cancer J82 Cells through Oxidative Stress [ Antioxidants (Basel), 2021, 10(7)1063]	PubMed: 34209212
The Activin/FLRG pathway associates with poor COVID-19 outcomes in hospitalized patients [ Mol Cell Biol, 2021, MCB0046721]	PubMed: 34723652
Activin A correlates with the worst outcomes in COVID-19 patients, and can be induced by cytokines via the IKK/NF-kappa B pathway [ bioRxiv, 2021, 10.1101/2021.02.04.429815]	PubMed: N/A
Low Concentration of Withaferin a Inhibits Oxidative Stress-Mediated Migration and Invasion in Oral Cancer Cells [ Biomolecules, 2020, 10(5)E777]	PubMed: 32429564
Withaferin A Induces Oxidative Stress-Mediated Apoptosis and DNA Damage in Oral Cancer Cells [ Front Physiol, 2017, 8:634]	PubMed: 28936177
Synergistic inhibition of glioma cell proliferation by Withaferin A and tumor treating fields [ J Neurooncol, 2017, 134(2):259-268]	PubMed: 28681243
AshwaMAX and Withaferin A inhibits gliomas in cellular and murine orthotopic models [ J Neurooncol, 2016, 126(2):253-64]	PubMed: 26650066

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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