Withaferin A
(Synonyms: 醉茄素A) 目录号 : GC17309A steroidal lactone with diverse biological activities
Cas No.:5119-48-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: |
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]. |
Animal experiment: |
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]. |
References: [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. |
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 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].
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].
References:
[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.
[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.
[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.
Cas No. | 5119-48-2 | SDF | |
别名 | 醉茄素A | ||
化学名 | (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 | ||
分子式 | C28H38O6 | 分子量 | 470.6 |
溶解度 | DMF: 5 mg/ml,DMSO: 5 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | 储存条件 | 4°C, protect from light |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1249 mL | 10.6247 mL | 21.2495 mL |
5 mM | 0.425 mL | 2.1249 mL | 4.2499 mL |
10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。