Home >> Bay 11-7821(BAY 11-7082)
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Bay 11-7821(BAY 11-7082) IKK/NF-κB/TNFα inhibitor

Catalog No.A4210
Size Price Stock Qty
10mg
$60.00
In stock
25mg
$120.00
In stock
50mg
$190.00
In stock
100mg
$300.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.

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Chemical structure

Bay 11-7821

Related Biological Data

Bay 11-7821

Related Biological Data

Bay 11-7821

Biological Activity

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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Chemical Properties

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 ≥64mg/mL in DMSO 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.

Background

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.