| Bay 11-7821(BAY 11-7082) IKK/NF-κB/TNFα inhibitor |
Sample solution is provided at 25 µL, 10mM.
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| Description | Bay 11-7821 is an inhibitor of E2 ubiquitin (Ub) conjugating enzyme and NF-κB. | |||||
| Targets | E2 ubiquitin conjugating enzyme | NF-κB | ||||
| IC50 | 10 μM | |||||
Bay 11-7821(BAY 11-7082) Dilution Calculator
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| Cas No. | 19542-67-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile | ||
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)C=CC#N | ||
| Formula | C10H9NO2S | M.Wt | 207.25 |
| Solubility | ≥64 mg/mL in DMSO, ≥10.64 mg/mL in EtOH with ultrasonic and warming, <2.46 mg/mL in H2O | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Bay 11-7821(Bay 11-7082) is an inhibitor of IKK with IC50 value of 10μM [1].
Bay 11-7821 inhibits the TNFα-induced phosphorylation of IκB-α, results in an inhibition of NF-κB. This subsequently causes the inhibition of the TNFα-induced surface expression of E-selectin, VCAM-1, and ICAM-1. It is reported that, Bay 11-7821 does not inhibit entire TNFα-induced phosphorylation but selectively inhibits phosphorylation of IκB-α [1].
Experiments show that Bay 11-7821 is highly toxic at concentrations of effective IKK inhibition. It can induce cell necrosis in MM cells. Additionally, Bay 11-7821 is proved to have an anti-inflammatory ability via inducing death of B-cell lymphoma and leukaemic T-cell. It is also reported to inhibit the NALP3 inflammasome in macrophages [2, 3].
References:
[1] Pierce JW, Schoenleber R, Jesmok G, Best J, Moore SA, Collins T, Gerritsen ME. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.
[2] Rauert-Wunderlich H1, Siegmund D, Maier E, Giner T, Bargou RC, Wajant H, Stühmer T. The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors. PLoS One. 2013;8(3):e59292.
[3] Strickson S1, Campbell DG, Emmerich CH, Knebel A, Plater L, Ritorto MS, Shpiro N, Cohen P. The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system. Biochem J. 2013 May 1;451(3):427-37.