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Withaferin A (Synonyms: NSC 101088, NSC 273757)

Catalog No.GC17309 Copy One-Click Copy Product Info

Withaferin A is a steroidal lactone generally obtained from Withania somnifera (L.) Dunal, commonly known as Ashwagandha.

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Withaferin A Chemical Structure

Cas No.: 5119-48-2

Size Price Stock Qty
10mM (in 1mL DMSO)
$232.00
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1mg
$104.00
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5mg
$224.00
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10mg
$368.00
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Sample solution is provided at 25 µL, 10mM.



Description of Withaferin A

Withaferin A is a steroidal lactone generally obtained from Withania somnifera (L.) Dunal, commonly known as Ashwagandha[1]. Withaferin A can inhibits NF-κB at a very low concentration in endothelial cells[2] and exhibits a broad spectrum of biological activities, including antioxidant, anti-inflammatory, antibacterial, antistress, cardioprotective, neuroprotective, and anticancer activities[3]. Withaferin A is commonly utilized in cancer research due to its anticancer activities against various cancer cell lines and preclinical cancer models, achieved by modulating the expression and activity of different oncogenic proteins[4].

Withaferin A potently inhibited cell proliferation in human MPM cells, treatment with Withaferin A at 5µM for 72h significantly inhibit cell growth[5]. In MCF-7 cells, treatment with Withaferin A at 2.5µM for 24h can increase in the level of total as well as S15 phosphorylated p53, which has been implicated in apoptosis induction[6].

Withaferin A (4mg/kg; 14d; i.p.) treatment can inhibits Isoproterenol-induced myocardial fibrosis in mice and significantly reduce heart necrosis[7]. Treatment with Withaferin A (4mg/kg; 10d; i.p.) significantly reduced murine solid tumour growth and improved survival rate of tumour bearing mice[8].

References:
[1]. Paul S, Chakraborty S, Anand U, et al. Withania somnifera (L.) Dunal (Ashwagandha): A comprehensive review on ethnopharmacology, pharmacotherapeutics, biomedicinal and toxicological aspects. Biomed Pharmacother. 2021 Nov;143:112175. doi: 10.1016/j.biopha.2021.112175. Epub 2021 Sep 27. PMID: 34649336.
[2]. Mohan R, Hammers HJ, Bargagna-Mohan P, et al. Withaferin A is a potent inhibitor of angiogenesis. Angiogenesis. 2004;7(2):115-22. doi: 10.1007/s10456-004-1026-3. PMID: 15516832.
[3]Tewari D, Chander V, Dhyani A, et al. Withania somnifera (L.) Dunal: Phytochemistry, structure-activity relationship, and anticancer potential. Phytomedicine. 2022 Apr;98:153949. doi: 10.1016/j.phymed.2022.153949. Epub 2022 Jan 19. PMID: 35151215.
[4]. Kumar S, Mathew SO, Aharwal RP, et al. Withaferin A: A Pleiotropic Anticancer Agent from the Indian Medicinal Plant Withania somnifera (L.) Dunal. Pharmaceuticals (Basel). 2023 Jan 22;16(2):160. doi: 10.3390/ph16020160. PMID: 37259311; PMCID: PMC9966696.
[5]. Yang H, Wang Y, Cheryan VT, et al. Withaferin A inhibits the proteasome activity in mesothelioma in vitro and in vivo. PLoS One. 2012;7(8):e41214. doi: 10.1371/journal.pone.0041214. Epub 2012 Aug 17. PMID: 22912669; PMCID: PMC3422308.
[6]. Hahm ER, Lee J, Huang Y, et al. Withaferin a suppresses estrogen receptor-α expression in human breast cancer cells. Mol Carcinog. 2011 Aug;50(8):614-24. doi: 10.1002/mc.20760. Epub 2011 Mar 22. PMID: 21432907; PMCID: PMC3129407.
[7]. Challa AA, Vukmirovic M, Blackmon J, et al. Withaferin-A reduces type I collagen expression in vitro and inhibits development of myocardial fibrosis in vivo. PLoS One. 2012;7(8):e42989. doi: 10.1371/journal.pone.0042989. Epub 2012 Aug 10. PMID: 22900077; PMCID: PMC3416765.
[8]. Abeesh P, Vishnu WK, Guruvayoorappan C. Preparation and characterization of withaferin A loaded pegylated nanoliposomal formulation with high loading efficacy: In vitro and in vivo anti-tumour study. Mater Sci Eng C Mater Biol Appl. 2021 Sep;128:112335. doi: 10.1016/j.msec.2021.112335. Epub 2021 Jul 27. Erratum in: Mater Sci Eng C Mater Biol Appl. 2021 Nov;130:112432. doi: 10.1016/j.msec.2021.112432. PMID: 34474886.

Protocol of Withaferin A

Cell experiment [1]:

Cell lines

MPM

Preparation Method

MPM cells were treated with 5µM dose of Withaferin A for 72h. Then viable/live cells were determined by MTT assay to evaluate cell proliferation.

Reaction Conditions

5µM; 72h

Applications

Withaferin A treatment inhibits MPM cell proliferation.
Animal experiment [2]:

Animal models

129 Svev male mice

Preparation Method

Isoproterenol (50mg/kg) was injected subcutaneously into 129 Svev male mice for 2 consecutive days, while Withaferin A (4mg/kg) was administered intraperitoneally daily for 14 days. 24h after the last injection, hearts were removed, weighed, fixed and processed for histopathologic analysis.

Dosage form

4mg/kg; 14d; i.p.

Applications

Withaferin A was greatly reduced Isoproterenol-induced heart necrosis compared to animals treated with Isoproterenol alone.

References:
[1]. Yang H, Wang Y, Cheryan VT, et al. Withaferin A inhibits the proteasome activity in mesothelioma in vitro and in vivo. PLoS One. 2012;7(8):e41214. doi: 10.1371/journal.pone.0041214. Epub 2012 Aug 17. PMID: 22912669; PMCID: PMC3422308.
[2]. Challa AA, Vukmirovic M, Blackmon J, et al. Withaferin-A reduces type I collagen expression in vitro and inhibits development of myocardial fibrosis in vivo. PLoS One. 2012;7(8):e42989. doi: 10.1371/journal.pone.0042989. Epub 2012 Aug 10. PMID: 22900077; PMCID: PMC3416765.

Chemical Properties of Withaferin A

Cas No. 5119-48-2 SDF
Synonyms NSC 101088, NSC 273757
Chemical Name (4S,4aR,5aR,6aS,6bS,9R,9aS,11aS,11bR)-4-hydroxy-9-((S)-1-((R)-5-(hydroxymethyl)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)ethyl)-9a,11b-dimethyl-5a,6,6a,6b,7,8,9,9a,10,11,11a,11b-dodecahydrocyclopenta[1,2]phenanthro[8a,9-b]oxiren-1(4H)-one
Canonical SMILES O[C@@H](C=C1)[C@@]23O[C@@H]2C[C@@H]([C@H]4[C@@]5(C)[C@@H]([C@H](C)[C@@H](CC(C)=C6CO)OC6=O)CC4)[C@H](CC5)[C@]3(C1=O)C
Formula C28H38O6 M.Wt 470.6
Solubility DMF: 5 mg/ml, DMSO:50mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Withaferin A

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1249 mL 10.6247 mL 21.2495 mL
5 mM 425 μL 2.1249 mL 4.2499 mL
10 mM 212.5 μL 1.0625 mL 2.1249 mL
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In vivo Formulation Calculator (Clear solution) of Withaferin A

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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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for Withaferin A

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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