Bay 11-7085
(Synonyms: (2E)-3-[[4-叔丁基苯基]磺酰基]-2-丙烯腈,BAY 11-7083) 目录号 : GC10345
An irreversible inhibitor of IκBα phosphorylation
Cas No.:196309-76-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
ECSCs and NESCs |
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Preparation method |
The solubility of this compound in DMSO is > 12.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.01 ~ 10 μM; |
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Applications |
In ECSCs and NESCs, BAY 11-7085 significantly inhibited cell viability in a dose-dependent manner. At the dose of 10 μM, ECSCs and NESCs treated with BAY 11-7085 showed 66.1% and 54.7% decreases in cell viability, respectively. In addition, according to the results of the BrdU incorporation assay, at the dose of 10 μM, BAY 11-7085 significantly inhibited the BrdU incorporation of ECSCs in a dose-dependent manner (53.2% decrease), whereas BAY 11-7085 only showed a weak inhibitory effect on the BrdU incorporation of NESCs (38.2% decrease). Therefore, BAY 11-7085 showed stronger inhibitory effects on the cell viability and the cell proliferation of ECSCs than on those of NESCs. |
| Animal experiment [2]: | |
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Animal models |
Rat model of pneumococcal meningitis |
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Dosage form |
20 mg; i.p. |
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Applications |
In rat model of pneumococcal meningitis, BAY 11-7085 significantly reduced meningitis-associated loss of cerebrovascular autoregulation. Besides, also BAY 11-7085 also significantly reduced increases in CSF WBCs, ICP and BBB permeability caused by pneumococcal infection. The results of Western blot analysis showed BAY 11-7085 inhibited meningitis-associated increase in NF-κB activity. |
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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]. Nasu K1, Nishida M, Ueda T, Yuge A, Takai N, Narahara H. Application of the nuclear factor-kappaB inhibitor BAY 11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23 [2]. Koedel U, Bayerlein I, Paul R, Sporer B, Pfister HW. Pharmacologic interference with NF-kappaB activation attenuates central nervous system complications in experimental Pneumococcal meningitis. J Infect Dis. 2000 Nov;182(5):1437-45. | |
BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
BAY 11-7085 inhibits TNFa-induced surface expression of E-selectin, VCAM-1, and ICAM-1with IC50 values in the range of 5-10 μM. BAY 11-7085 stabilizes IκBα in a dose-dependent manner with an IC50 value of approximately 10 μM. There is a clear correlation between the concentration of drug that stabilized IκBα, the concentration that inhibits nuclear levels of NF-kB, and the concentration that inhibits adhesion molecule expression[1]. BAY 11-7085 has been shown to inhibit cell proliferation and induce apoptosis of a variety of cells. BAY 11-7085 (ECSCs) significantly inhibits the cell proliferation and DNA synthesis of ovarian endometriotic cyst stromal cells and induces apoptosis and the G0/G1 phase cell cycle arrest of these cells. BAY 11-7085 induces apoptosis of ECSCs by suppressing antiapoptotic proteins, and that caspase-3-, -8-, and -9-mediated cascades are involved in this mechanism[2].
BAY 11-7085 acts as an anti-inflammatory agent in both the rat carrageenan paw and the rat adjuvant arthritis model. It demonstrates a dose-dependent reduction in swelling in the rat carrageenan paw model[1].
References:
[1]. Pierce JW, et al. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesionmolecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.
[2]. Nasu K, et al. Application of the nuclear factor-kappaB inhibitor BAY 11-7085 for the treatment of endometriosis: an in vitro study. Am J Physiol Endocrinol Metab. 2007 Jul;293(1):E16-23.
| Cas No. | 196309-76-9 | SDF | |
| 别名 | (2E)-3-[[4-叔丁基苯基]磺酰基]-2-丙烯腈,BAY 11-7083 | ||
| 化学名 | (E)-3-(4-tert-butylphenyl)sulfonylprop-2-enenitrile | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N | ||
| 分子式 | C13H15NO2S | 分子量 | 249.33 |
| 溶解度 | ≥ 12.45mg/mL in DMSO | 储存条件 | Store at -20° 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0107 mL | 20.0537 mL | 40.1075 mL |
| 5 mM | 0.8021 mL | 4.0107 mL | 8.0215 mL |
| 10 mM | 0.4011 mL | 2.0054 mL | 4.0107 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。