Bay 11-7085 |
| Catalog No.GC10345 |
NK-κB activation inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 196309-76-9
Sample solution is provided at 25 µL, 10mM.
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.
| 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. | |
| Cas No. | 196309-76-9 | SDF | |
| Chemical Name | (E)-3-(4-tert-butylphenyl)sulfonylprop-2-enenitrile | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N | ||
| Formula | C13H15NO2S | M.Wt | 249.33 |
| Solubility | ≥ 12.45mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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