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Bay 11-7821(BAY 11-7082)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Bay 11-7821(BAY 11-7082)图片
CAS NO:19542-67-7
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

化学性质

StorageStore at -20°C
M.Wt207.25
Cas No.19542-67-7
FormulaC10H9NO2S
Solubilityinsoluble in H2O; ≥64 mg/mL in DMSO; ≥10.64 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name(E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)C=CC#N
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Bay 11-7821（Bay 11-7082）是IKK的抑制剂，其IC50值为10 μM[1]。

Bay 11-7821可抑制TNFα诱导的IκB-α磷酸化，从而抑制NF-κB，进而抑制TNFα诱发的E-选择素、VCAM-1和ICAM-1的表面表达。据报道，Bay 11-7821并不抑制全部TNFα诱导的磷酸化，只选择性地抑制IκB-α的磷酸化[1]。

实验显示，Bay 11-7821在有效抑制IKK的浓度下具有高毒性。在MM细胞中可抑制细胞坏死。此外，Bay 11-7821通过诱导B细胞淋巴瘤和白血病T细胞的死亡，从而具有抗炎作用。据报道，Bay 11-7821可抑制巨噬细胞中的NALP3炎性复合体[2, 3]。

参考文献：
[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.

试验操作

Cell experiment:[1]

Cell lines

Non-small cell lung cancer cell line NCI-H1703

Reaction Conditions

0 ~ 8 μM Bay 11-7821 for 12 h incubation

Applications

Bay 11-7821 (< 8 μM) was able to effectively inhibit both basal and TNFα stimulated NF-κB luciferase activity in a dose dependent manner. Bay 11-7821 (8 μM) strongly inhibited the rate of proliferation in NCI-H1703 cells.

Animal experiment:[2]

Animal models

Mice xenografted with human gastric cancer HGC27 cells

Dosage form

2.5 or 5 mg/kg

Twice-weekly intratumoral injection of Bay 11-7821, for 21 days

Applications

Treatment of Bay 11-7821 significantly suppressed tumor growth in a dose-dependent manner. Furthermore, Bay 11-7821 dose-dependently induced cellular apoptosis and inhibited proliferation in tumor xenografts.

Note

The technical data provided above is for reference only.

References:

1. Gastonguay A, Berg T, Hauser AD, et al. The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma. Cancer Biology & Therapy, 2012, 13(8): 647-656.

2. Chen L, Ruan Y, Wang X, et al. BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells. Journal of Gastroenterology, 2014, 49(5): 864-874.

生物活性

描述Bay 11-7821是E2泛素（Ub）连接酶和NF-κB的抑制剂。
靶点E2 ubiquitin conjugating enzymeNF-κB    
IC50 10 μM