Wedelolactone
(Synonyms: 蟛蜞菊内酯) 目录号 : GN10269
A natural NF-κB inhibitor
Cas No.:524-12-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Mouse BALB/c 3T3 cells, mouse splenocytes from C57/B6 mice, HeLa cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 h, 0~100 µM |
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Applications |
In cultured mouse BALB/c 3T3 cells, mouse splenocytes and HeLa cells, wedelolactone (0~100 µM) inhibited LPS-induced caspase-11 expression by inhibiting NF-κB-mediated transcription through the direct inhibition of IKK. In BALB/c 3T3 cells and/or HeLa cells, wedelolactone inhibited the endogenous IKK activity at 50 µM, the phosphorylation as well as degradation of IκBα at 100 µM, NF-κB transcriptional activity and the LPS-induced caspase-11 mRNA expression at 60 µM. In mouse splenocytes, wedelolactone (50 µM and 100 µM) also inhibited the secretion of the proinflammatory cytokine IL-1β, which maturated by caspase-11-activated caspase-1. |
| Animal experiment [2]: | |
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Animal models |
Swiss albino male mice |
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Dosage form |
Wedelolactone 10 μM in 200 μl acetone 1 h before and after every UVB exposure (0.42 J/m2 for 6 h), three weekly for 21 days |
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Application |
On Swiss albino male mouse skin, IKK inhibition by wedelolactone (10 μM) produced profound effect on several molecular targets of UVB induced cell signaling, including GSH, GST, GPx, LPO, CAT, MPO, NO, cGMP, PKC, NF-κB, COX-2, VEGF, etc. Wedelolactone prevented the induction of NF-κB, and thereby limited inflammation and modulated cell environment to a non-persuasive state for neoplastic transformation, and also limited the reactive oxygen species generation following UVB exposure. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Kobori M, Yang Z, Gong D, et al. Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK complex.[J]. Cell Death & Differentiation, 2004, 11(1):123-30. [2] Ali F, Khan B A, Sultana S. Wedelolactone mitigates UVB induced oxidative stress, inflammation and early tumor promotion events in murine skin: plausible role of NFκB pathway[J]. European Journal of Pharmacology, 2016, 786:253-264. |
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Wedelolactone is an inhibitor of IKK.
IkB kinase (IKK) complex contains the catalytic subunits IKKα and IKKβ, and the regulatory subunit IKKγ/NEMO. IKK, is a kinase critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. The induction of caspase-11 is an important upstream controlling event in inflammatory response and apoptosis under pathological conditions modulated by upstream NF-κB-mediated transcription[1].
In vitro: In cultured mouse BALB/c 3T3 cells, mouse splenocytes and HeLa cells, wedelolactone (0~100 μM) inhibited LPS-induced caspase-11 expression by inhibiting NF-κB-mediated transcription through the direct inhibition of IKK. Wedelolactone played an potential role in anti-inflammatory therapy to inhibit IL-1β levels in diseases such as rheumatoid arthritis, asthma and septic shock[1].
In vivo: On Swiss albino male mouse skin, IKK inhibition by wedelolactone (10 μM) prevented the induction of NF-κB, perturbed the generation of reactive oxygen species and reactive nitrogen intermediates, blunted the signal transduction that lead to the activation of the early immediate genes, and thereby protected mouse skin from the UVB induced neoplastic transformation, angiotropism and metastatic progression [2].
References:
[1] Kobori M, Yang Z, Gong D, et al. Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK complex.[J]. Cell Death & Differentiation, 2004, 11(1):123-30.
[2] Ali F, Khan B A, Sultana S. Wedelolactone mitigates UVB induced oxidative stress, inflammation and early tumor promotion events in murine skin: plausible role of NFκB pathway[J]. European Journal of Pharmacology, 2016, 786:253-264.
| Cas No. | 524-12-9 | SDF | |
| 别名 | 蟛蜞菊内酯 | ||
| 化学名 | 1,8,9-trihydroxy-3-methoxy-[1]benzofuro[3,2-c]chromen-6-one | ||
| Canonical SMILES | COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O | ||
| 分子式 | C16H10O7 | 分子量 | 314.25 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL,Ethanol: 20 mg/mL | 储存条件 | Store at 2-8°C |
| 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 | 3.1822 mL | 15.9109 mL | 31.8218 mL |
| 5 mM | 0.6364 mL | 3.1822 mL | 6.3644 mL |
| 10 mM | 0.3182 mL | 1.5911 mL | 3.1822 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。