Bay 11-7821
(Synonyms: BAY 11-7082) 目录号 : GC13035A selective and irreversible NF-κB inhibitor
Cas No.:19542-67-7
Sample solution is provided at 25 µL, 10mM.
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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].
Bay 11-7821(Bay 11-7082)是一种IKK抑制剂,其IC50值为10μM[1]。
Bay 11-7821抑制TNFα诱导的IκB-α磷酸化,导致NF-κB的抑制。这随后导致TNFα诱导的E-selectin、VCAM-1和ICAM-1的表面表达受到抑制。有报道称,Bay 11-7821并不完全抑制TNFα诱导的磷酸化,而是选择性地抑制IκB-α的磷酸化[1]。
实验表明,Bay 11-7821在有效抑制IKK的浓度下具有很高的毒性。它可以在多发性骨髓瘤细胞中诱导细胞坏死。此外,Bay 11-7821被证明具有抗炎能力,可以诱导B细胞淋巴瘤和白血病T细胞的死亡。有报道称它还可以抑制巨噬细胞中的NALP3炎症小体[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.
Cas No. | 19542-67-7 | SDF | |
别名 | BAY 11-7082 | ||
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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.8251 mL | 24.1255 mL | 48.2509 mL |
5 mM | 0.965 mL | 4.8251 mL | 9.6502 mL |
10 mM | 0.4825 mL | 2.4125 mL | 4.8251 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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