Bay 11-7085
BAY 11-7085 is a soluble inhibitor of NK-κB activation [1].
BAY 11-7085 has been reported to inhibit cell proliferation and induce cell apoptosis in a variety of cells. In addition, BAY 11-7085 has been revealed to inhibit DNA synthesis of ECSCs and induce the G0/G1 phase cell cycle arrest. Moreover, BAY 11-7085 has shown to induce cell apoptosis by inhibiting anti-apoptotic proteins. After treatment with BAY 11-7085, down-regulations of the B-cell lymphoma/leukemia-2 (Bcl-2) and Bcl-XL expressions with simultaneous activations of caspase-3, caspase-8, and caspase-9 were observed in ECSCs. [1].
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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 249.33 |
| Cas No. | 196309-76-9 |
| Formula | C13H15NO2S |
| Solubility | ≥12.45 mg/mL in DMSO |
| Chemical Name | (E)-3-(4-tert-butylphenyl)sulfonylprop-2-enenitrile |
| SDF | Download SDF |
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)C=CC#N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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. |
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| Description | BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with an IC50 value of 10 μM. | |||||
| Targets | IκBα?phosphorylation | |||||
| IC50 | 10 μM | |||||
Quality Control & MSDS
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Chemical structure
