| CAS NO: | 19542-67-7 |
| 包装 | 价格(元) |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| Storage | Store at -20°C |
| M.Wt | 207.25 |
| Cas No. | 19542-67-7 |
| Formula | C10H9NO2S |
| Solubility | insoluble 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 SMILES | CC1=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。 |
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.
| 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. | |
| 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 enzyme | NF-κB | ||||
| IC50 | 10 μM | |||||
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