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BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
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Source | Clin Exp Otorhinolaryngol (2018). Figure 3. Bay 11-7085 |
| Method | RT-PCR | |
| Cell Lines | B cells | |
| Concentrations | 10 μM | |
| Incubation Time | 1 h | |
| Results | Results of RT-PCR and ELISA showed that BAY 11-7085 significantly attenuated recombinant nCLU-induced MUC5AC mRNA expression and protein production |
| Cell Experiment | |
|---|---|
| Cell lines | HUVEC |
| Preparation method | Human umbilical vein endothelial cells (HUVEC) were isolated and maintained in culture using previously described procedures. For experiments on cytokine induction, cells were exposed to recombinant human TNFα at a final concentration of 100 units/ml in complete media for the times indicated. The proteosomal inhibitor carbobenzoxyl-leucinyl-leucinyl-leucinal-H (MG115) was prepared as a 40 mM stock solution in Me2SO and added to complete medium to a final concentration of 40 μM. Cell toxicity was assessed by morphology and by 3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. |
| Concentrations | 0, 1.25, 2.5, 5, 10 and 20 μM |
| Incubation time | 16 h |
| Animal Experiment | |
|---|---|
| Animal models | male Lewis rats of Adjuvant Arthritis model |
| Formulation | 0.5% methyl cellulose |
| Dosages | 5 or 20 mg/kg once a day |
| Administration | intraperitoneal injection |
| Molecular Weight | 249.33 |
| Formula | C13H15NO2S |
| CAS Number | 196309-76-9 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IκB/IKK Products |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| SC-514
SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) with IC50 of 3-12 μM. |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
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