| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Withaferin A, a steroidal lactone class of NFkB/IkB Inhibitor, is a natural product extracted from Acnistus arborescens, Withania somnifera (Indian Winter cherry or Ashwagandha in Sanskrit) and other members of Solanaceae family. Ayurvedic medicine has historically used it. It is the earliest discovered ergostane-type product belonging to the withanolide class. This natural product has a wide range of pharmacological properties, including cardioprotective, anti-inflammatory, immuno-modulatory, anti-angiogenesis, anti-metastasis, and anti-carcinogenic properties.
| Targets |
NF-κB; vimentin
|
|---|---|
| ln Vitro |
Withaferin A inhibits NF-kB activation effectively and has anti-inflammatory properties by preventing Ik-B kinase beta from being activated by TNF through a thioalkylation-sensitive redox mechanism[1].
Withaferin A has anticancer properties as well. The IF protein vimentin is the target of withaferin A, which also causes vimentin filaments to aggregate in bovine aortic endothelial cells (BAECs) at 3 μM and fragment in endothelial cells at 10 μM[2]. The tumorigenic potential of ALDH1 positive cancer stem cells (CSCs) is decreased in a dose-dependent manner by withaferin A (0.5, 1.5 μM) alone or in combination with cisplatin (CIS)[3]. |
| ln Vivo |
In mice, withaferin A (2 mg/kg, i.p.) exhibits strong angiogenesis inhibitory activity through vimentin[2]. In tumors taken from mice, the combination of withaferin A (2 mg/kg) and cisplatin (CIS) controls the expression of the ALDH1 marker and inhibits the expression of securin[3].
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| Cell Assay |
The RPMI1640 medium is used to support the ovarian epithelial cancer cell line A2780. It also contains insulin (5 g/mL), penicillin/streptomycin (100 IU/mL and 100 g/mL, respectively), and 10% fetal bovine serum (FBS) from Hyclone. In DMSO, other reagents such as withaferin A and cisplatin (CIS) are prepared. Each time it is made, cisplatin is fresh[3].
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| Animal Protocol |
Mice: In the assay, mice with either a vimentin homozygous defect (Vim−/−) or a vimentin heterozygous defect (Vim−/−) on the 129/Svev background are used. The intraperitoneal (i.p.) injection of ketamine and xylazine is used to anesthetize mice between the ages of 4 and 6 weeks. Proparacain eye drop is used to topically anesthetize the corneas before 1 μL of diluted sodium hydroxide solution (0.15 M) is applied for 1 minute. The cornea is immediately thoroughly washed in saline solution, followed by the delicate removal of the corneal and limbal epithelium by scraping. Atropine eye drops are used topically to treat the cornea, and antibiotic eye ointments containing tobramycin and erythromycin are used to protect it. In the drug or control groups of mice, withaferin A or 12-D WS (2 mg/kg solubilized in DMSO) or vehicle (DMSO) are injected intraperitoneally (i.p.) after the mice have recovered from corneal injury, and then once a day for the following ten days. Eyes are removed from mice that have been killed humanely. In order to prepare the corneal buttons, the anterior segment of the eyes is divided in half. Corneal tissues are fixed in 100% acetone for 20 minutes, cleaned in PBS for 1 hour, and blocked for 18 hours at 4°C in 1% BSA-PBS. Cornea whole-mount staining involves soaking tissues in FITC-conjugated rat anti-mouse CD31 antibody (1:333 dilution in 1% BSA-PBS) for 12 hours, rinsing them off for 24 hours at 4°C in the same solution, and attaching them to glass slides with coverslips. By importing digital images into NIH ImageJ, fluorescent staining can be quantified after being visualized on a microscope[2].
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| References |
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| Molecular Formula |
C28H38O6
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|---|---|
| Molecular Weight |
470.5977
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| Exact Mass |
470.27
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| Elemental Analysis |
C, 71.46; H, 8.14; O, 20.40
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| CAS # |
5119-48-2
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| Related CAS # |
5119-48-2
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| Appearance |
White to off-white solid powder
|
| SMILES |
CC1=C(C(=O)O[C@H](C1)[C@@H](C)[C@H]2CC[C@@H]3[C@@]2(CC[C@H]4[C@H]3C[C@@H]5[C@]6([C@@]4(C(=O)C=C[C@@H]6O)C)O5)C)CO
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| InChi Key |
DBRXOUCRJQVYJQ-CKNDUULBSA-N
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| InChi Code |
InChI=1S/C28H38O6/c1-14-11-21(33-25(32)17(14)13-29)15(2)18-5-6-19-16-12-24-28(34-24)23(31)8-7-22(30)27(28,4)20(16)9-10-26(18,19)3/h7-8,15-16,18-21,23-24,29,31H,5-6,9-13H2,1-4H3/t15-,16-,18+,19-,20-,21+,23-,24+,26+,27-,28+/m0/s1
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| Chemical Name |
(1S,2R,6S,7R,9R,11S,12S,15R,16S)-6-hydroxy-15-[(1S)-1-[(2R)-5-(hydroxymethyl)-4-methyl-6-oxo-2,3-dihydropyran-2-yl]ethyl]-2,16-dimethyl-8-oxapentacyclo[9.7.0.02,7.07,9.012,16]octadec-4-en-3-one
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| Synonyms |
NSC 101088; NSC101088; NSC-101088; NSC-273757; NSC273757; NSC 273757; Withaferin A
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~94 mg/mL (106.3~199.75 mM)
Ethanol: ~4 mg/mL (~8.50 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1249 mL | 10.6247 mL | 21.2495 mL | |
| 5 mM | 0.4250 mL | 2.1249 mL | 4.2499 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05610735 | Not yet recruiting | Drug: DOXIL Drug: Withaferin A |
Recurrent Ovarian Cancer | Sham Sunder Kakar | August 1, 2023 | Phase 1 Phase 2 |
Products are for research use only; We do not sell to patients
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