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Bay 11-7821 目录号 GC13035

IKK/NF-κB/TNFα inhibitor

规格 价格 库存 购买数量
10mg
¥410.00
现货
25mg
¥819.00
现货
50mg
¥1,470.00
现货
100mg
¥2,195.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 19542-67-7 SDF
别名 N/A
化学名 (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
Canonical SMILES CC1=CC=C(C=C1)S(=O)(=O)C=CC#N
分子式 C10H9NO2S 分子量 207.25
溶解度 ≥ 64 mg/mL in DMSO, ≥ 10.64 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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.