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Bay 11-7821(BAY 11-7082)
IKK/NF-κB/TNFα抑制剂,BAY 11-7082是 NF-κB 抑制剂, 其通过抑制TNF-α诱导的IκB-α磷酸化来降低NF-κB。 BAY 11-7082抑制泛素化蛋白酶 USP7 和 USP21 的 IC50 分别为0.19 μM 和 0.96 μM。
目录号: PC11540 纯度: ≥98%
CAS No. :19542-67-7
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中文名称
Bay 11-7821(BAY 11-7082)
中文别名
(E)-3-(对甲苯磺酰基)丙烯腈;(2E)-3-[(4-甲基苯基)磺酰基]-2-丙烯腈;(E)-3-(p-Toluenesulfonyl)acrylonitrile (E)-3-(对甲苯磺酰基)丙烯腈;(E)-3-(p-甲苯磺酰基)丙烯腈;7-甲基-1H-吲哚-4-醇;BAY11-7082 抑制剂;NF-κB抑制剂BAY 11-7082;(E)-3-甲苯磺酰基丙烯腈
英文名称
Bay 11-7821(BAY 11-7082)
英文别名
(E)-3-Tosylacrylonitrile;BAY 11-7082;(E)?-?3-?(p-?Toluenesulfonyl)?acrylonitrile;(E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile;(E)-3-(P-TOLUENESULFONYL)ACRYLONITRILE;Bay 11-7082 (Bay 11-7821);BAY 11-7821;BAY-11-7082;(E)-3-(4-Methylphenylsulfonyl)-2-propenenitrile;BAY 117821;BAY11-7082,BAY 117821;(E)-3-(p-tolylsulfonyl)prop-2-enenitrile;(2E)-3-[(4-METHYLPHENYL)SULFONYL]-2-PROPENENITRILE;BAY117082;4Y5G2A4F6O;3-(4-methylphenylsulfonyl)-2-propenenitrile;3-[(4-methylphenyl)sulfonyl]prop-2-enenitrile;(E)3-[(4-Methylphenyl)sulfonyl]-2-propenenitrile;(2E)-3-[(4
Cas No.
19542-67-7
分子式
C10NO2SH9
分子量
207.25
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

性状

Solid

IC50 & Target[1][2]

NF-κB

 

USP7

0.19 μM (IC50)

USP21

0.96 μM (IC50)

Autophagy

 

体外研究(In Vitro)

BAY 11-7082 (BAY 11-7821), an inhibitor of NF-κB, induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells. Bay 11-7082 rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulated the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB. Bay 11-7082 selectively inhibits Tax-induced NF-κB activity in a human T-cell line. BAY 11-7082 inhibits NFκB signalling and is recently shown to inhibit the majority of E2 and E3 ligases tested by reacting covalently with the catalytic cysteine residues. Moreover, BAY 11-7082 also inhibits several tyrosine phosphatases by reacting with catalytic Cys residue of these enzymes. NSC 697923 is originally shown to inhibit the E2 ligase Ubc13-Uev1A. BAY 11-7082 inhibits the phosphorylation of IκBα and activation of NF-κB, induces the death of HBL-1 cells. BAY 11-7082 completely suppresses the LPS-stimulated and IL-1-stimulated phosphorylation of the activation loop of IKKβ. BAY 11-7082 acts by inhibiting TNF-α-induced phosphorylation of IκB-α, resulting in decreased NF-κB and decreases expression of adhesion molecules.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

BAY 11-7082 (2.5 mg/kg and 5 mg/kg; intratumoral injection; twice-weekly for 21 days ) significantly suppresses tumor growth in a dose-dependent manner.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four-week-old male BALB/c nude mice with human gastric carcinoma cell lines HGC-27
Dosage: Low-dose (2.5 mg/kg body weight), high-dose (5 mg/kg body weight)
Administration: Intratumoral injection; twice-weekly for 21 days
Result: Suppressed tumor growth in a dose-dependent manner.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 100 mg/mL (482.51 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.8251 mL 24.1255 mL 48.2509 mL
5 mM 0.9650 mL 4.8251 mL 9.6502 mL
10 mM 0.4825 mL 2.4125 mL 4.8251 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (12.06 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.06 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (12.06 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.06 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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