HY-N2065-1mg | Withaferin A [5119-48-2] Biotrend

Beschreibung

Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.

IC₅₀ & Target^[1]

NFκB

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	32.7 nM Compound: 1; WA	Antiproliferative activity against cisplatin-sensitive human A2780 cells measured after 96 hrs by MTT assay Antiproliferative activity against cisplatin-sensitive human A2780 cells measured after 96 hrs by MTT assay	[PMID: 31008605]
A549	IC₅₀	10.1 μM Compound: 1; WA	Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
A549	IC₅₀	6.6 μM Compound: 1; WA	Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
ACHN	IC₅₀	> 2000 nM Compound: 2a	Sensitization of TRAIL-induced apoptosis in human ACHN cells assessed as reduction in cell viability preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay Sensitization of TRAIL-induced apoptosis in human ACHN cells assessed as reduction in cell viability preincubated for 2 hrs followed by addition of TRAIL measured after 18 hrs by MTS assay	[PMID: 28257574]
ARPE-19	IC₅₀	37 nM Compound: 1; WA	Cytotoxicity against human ARPE19 cells measured after 96 hrs by MTT assay Cytotoxicity against human ARPE19 cells measured after 96 hrs by MTT assay	[PMID: 31008605]
BXPC-3	IC₅₀	2.78 μM Compound: 46; WA	Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay Antiproliferative activity against human BxPC3 cells after 48 hrs by MTS assay	[PMID: 31663736]
HCT-116	IC₅₀	3.7 μM Compound: 75	Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33445154]
HEK-293T	IC₅₀	299 nM Compound: 1	Cytotoxicity against human 293T cells assessed as reduction in cell viability after 72 hrs by resazurin dye based Alamar blue assay Cytotoxicity against human 293T cells assessed as reduction in cell viability after 72 hrs by resazurin dye based Alamar blue assay	[PMID: 29537263]
HeLa	IC₅₀	3 μM Compound: 1; WA	Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
HeLa	IC₅₀	6.3 μM Compound: 1; WA	Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
HFF	IC₅₀	> 6.8 μM Compound: 22	Cytotoxicity against human HFF cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human HFF cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
LNCaP	IC₅₀	0.87 μM Compound: 22	Cytotoxicity against human LNCAP cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human LNCAP cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
MCF7	IC₅₀	0.57 μM Compound: 22	Cytotoxicity against human MCF7 cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human MCF7 cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
MCF7	IC₅₀	1.3 μM Compound: 1; WA	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
MCF7	IC₅₀	3.6 μM Compound: 1; WA	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
MIA PaCa-2	IC₅₀	2.93 μM Compound: 46; WA	Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTS assay Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTS assay	[PMID: 31663736]
MM1.S	IC₅₀	53 nM Compound: 1	Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay	[PMID: 34445874]
Multiple myeloma cancer stem cell	IC₅₀	649.7 nM Compound: WFA	Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay	[PMID: 30108696]
NCI-H460	IC₅₀	< 0.4 μM Compound: 22	Cytotoxicity against human NCI-H460 cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human NCI-H460 cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
PANC-1	IC₅₀	1.24 μM Compound: 46; WA	Antiproliferative activity against human PANC1 cells after 48 hrs by MTS assay Antiproliferative activity against human PANC1 cells after 48 hrs by MTS assay	[PMID: 31663736]
PC-3M	IC₅₀	0.41 μM Compound: 22	Cytotoxicity against human PC3M cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human PC3M cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
RPMI-8226	IC₅₀	1.6 μM Compound: 1	Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay	[PMID: 34445874]
RPMI-8226	IC₅₀	258 nM Compound: 1	Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay	[PMID: 34445874]
SF-268	IC₅₀	< 0.4 μM Compound: 22	Cytotoxicity against human SF268 cells after 72 hrs by resazurin-based colorimetric assay Cytotoxicity against human SF268 cells after 72 hrs by resazurin-based colorimetric assay	[PMID: 27071003]
SW480	IC₅₀	4.9 μM Compound: 75	Anticancer activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Anticancer activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33445154]
Vero	IC₅₀	1.3 μM Compound: 1; WA	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]
Vero	IC₅₀	6.6 μM Compound: 1; WA	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay	[PMID: 28923386]

In Vitro

Withaferin A has antiinflammatory activity, and potently inhibits NF-kB activation by preventing the TNF-induced activation of Ik-B kinase beta via a thioalkylation-sensitive redox mechanism^[1].
Withaferin A also has anticancer activity. Withaferin A targets the IF protein vimentin, causes aggregation of vimentin filaments in bovine aortic endothelial cells (BAECs) at 3 μM, and induces vimentin fragmentation in endothelial cells at 10 μM^[2].
Withaferin A (0.5, 1.5 μM) alone or incombination with cisplatin (CIS) dose-dependently reduces tumorigenic potential of ALDH1 positive cancer stem cells (CSCs)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Withaferin A (2 mg/kg, i.p.) shows potent angiogenesis inhibitory activity via vimentin in mice^[2]. Withaferin A (2 mg/kg) combined with cisplatin (CIS) regulates the expression of ALDH1 marker, and downregulates the expression of securin in tumors collected from mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Klinische Studie

Molekulargewicht

470.60

Formel

C₂₈H₃₈O₆

CAS. Nr.

5119-48-2

Appearance

Solid

Color

White to off-white

SMILES

C[C@]([C@](CC[C@@]1(C)[C@@]2(06)CC[C@]1(06)[C@@H]([C@@](O3)(06)CC(C)=C(CO)C3=O)C)(06)[C@@]2(06)C4)(C(C=C5)=O)[C@@]6([C@H]5O)[C@@H]4O6

Structure Classification

Steroids

Initial Source

Plants
Solanaceae
Withania somnifera

Plants
other families

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (106.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner
Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (1.76 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (1.76 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (1.76 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.92%

Select Batch:

SDS (393 KB)

COA (254 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Kaileh M, et al. Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity. J Biol Chem. 2007 Feb 16;282(7):4253-64. Epub 2006 Dec 6. [Content Brief]

[2]. Bargagna-Mohan P, et al. The tumor inhibitor and antiangiogenic agent withaferin A targets the intermediate filament protein vimentin. Chem Biol. 2007 Jun;14(6):623-34. [Content Brief]

[3]. Kakar SS, et al. Withaferin A (WFA) inhibits tumor growth and metastasis by targeting ovarian cancer stem cells. Oncotarget. 2017 Aug 10;8(43):74494-74505. [Content Brief]

Zellassay ^[3]	Ovarian epithelial cancer cell line A2780 is maintained in RPMI1640 medium supplemented with insulin (5 μg/mL), penicillin/streptomycin (100 IU/mL and 100 μg/mL respectively) and 10% fetal bovine serum (FBS) from Hyclone. Withaferin A, cisplatin (CIS) and other reagents are prepared in DMSO. Cisplatin is prepared fresh each time^[3]. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[2]	Mice^[2] Vimentin homozygous-deficient mice (Vim^−/−) and mice that are vimentin-heterozygous deficient (Vim^+/−) in the 129/Svev background are used in the assay. In brief, mice between 4 and 6 wk of age are anesthetized by intraperiteoneal (i.p.) injection of ketamine and xylazine. Corneas are topically anesthetized by application of proparacain eye drop, and 1 μL drop of dilute 0.15 M sodium hydroxide is applied for 1 min. The cornea is immediately washed extensively in saline solution, and corneal and limbal epithelium gently removed by scraping. The cornea is topically treated with atropine eye drop and covered with tobramycin and erythromycin antibiotic eye ointment. Withaferin A or 12-D WS (2 mg/kg solubilized in DMSO) or vehicle (DMSO) is injected i.p. in respective drug or control groups of mice after their recovery from corneal injury, and subsequently every day thereafter for a period of 10 days. Mice are humanely killed and eyes enucleated. The anterior segment half of eyes are dissected and corneal buttons are prepared. Corneal tissues are fixed in 100% acetone for 20 min, washed in PBS for 1 hr, and blocked for 18 hr in 1% BSA-PBS at 4°C. Cornea whole-mount staining is performed by incubating tissues in FITC-conjugated rat anti-mouse CD31 antibody (1:333 dilution in 1% BSA-PBS) for 12 hr, washed away for 24 hr at 4°C in 1% BSA-PBS, and affixed to glass slides with a coverslip. Fluorescent staining is visualized on microscope, and quantified by importing digital images to NIH ImageJ^[2]. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise	[1]. Kaileh M, et al. Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity. J Biol Chem. 2007 Feb 16;282(7):4253-64. Epub 2006 Dec 6. [Content Brief] [2]. Bargagna-Mohan P, et al. The tumor inhibitor and antiangiogenic agent withaferin A targets the intermediate filament protein vimentin. Chem Biol. 2007 Jun;14(6):623-34. [Content Brief] [3]. Kakar SS, et al. Withaferin A (WFA) inhibits tumor growth and metastasis by targeting ovarian cancer stem cells. Oncotarget. 2017 Aug 10;8(43):74494-74505. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1249 mL	10.6247 mL	21.2495 mL	53.1237 mL
	5 mM	0.4250 mL	2.1249 mL	4.2499 mL	10.6247 mL
	10 mM	0.2125 mL	1.0625 mL	2.1249 mL	5.3124 mL
	15 mM	0.1417 mL	0.7083 mL	1.4166 mL	3.5416 mL
	20 mM	0.1062 mL	0.5312 mL	1.0625 mL	2.6562 mL
	25 mM	0.0850 mL	0.4250 mL	0.8500 mL	2.1249 mL
	30 mM	0.0708 mL	0.3542 mL	0.7083 mL	1.7708 mL
	40 mM	0.0531 mL	0.2656 mL	0.5312 mL	1.3281 mL
	50 mM	0.0425 mL	0.2125 mL	0.4250 mL	1.0625 mL
	60 mM	0.0354 mL	0.1771 mL	0.3542 mL	0.8854 mL
	80 mM	0.0266 mL	0.1328 mL	0.2656 mL	0.6640 mL
	100 mM	0.0212 mL	0.1062 mL	0.2125 mL	0.5312 mL

Withaferin A Related Classifications

Inflammation/Immunology Cancer
Cancer Targeted Therapy Cancer Immunotherapy Cancer Stem Cells Cancer Metabolism and Metastasis

NF-κB Apoptosis
NF-κB Ferroptosis

Withaferin A [5119-48-2]

Katalog-Nummer HY-N2065-1mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of Withaferin A:

Alle NF-κB Isoform-spezifische Produkte anzeigen:

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Withaferin A Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein:

Withaferin A [5119-48-2]

Katalog-Nummer HY-N2065-1mg

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Other Forms of Withaferin A:

Alle NF-κB Isoform-spezifische Produkte anzeigen:

Withaferin A Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Withaferin A Related Classifications

Keywords:

Sie könnten auch an folgenden Produkten interessiert sein: