Bay 11-7821（Bay 11-7082）是一種IKK抑制劑，其IC50值為10μM[1]。

Bay 11-7821抑制TNFα誘導(dǎo)的IκB-α磷酸化，導(dǎo)致NF-κB的抑制。這隨后導(dǎo)致TNFα誘導(dǎo)的E-selectin、VCAM-1和ICAM-1的表面表達(dá)受到抑制。有報(bào)道稱，Bay 11-7821并不完全抑制TNFα誘導(dǎo)的磷酸化，而是選擇性地抑制IκB-α的磷酸化[1]。

實(shí)驗(yàn)表明，Bay 11-7821在有效抑制IKK的濃度下具有很高的毒性。它可以在多發(fā)性骨髓瘤細(xì)胞中誘導(dǎo)細(xì)胞壞死。此外，Bay 11-7821被證明具有抗炎能力，可以誘導(dǎo)B細(xì)胞淋巴瘤和白血病T細(xì)胞的死亡。有報(bào)道稱它還可以抑制巨噬細(xì)胞中的NALP3炎癥小體[2，3]。

產(chǎn)品性質(zhì)：

Cas No.:19542-67-7

別名:BAY 11-7082

化學(xué)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

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

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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.