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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 11-7082图片
CAS NO:19542-67-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
Bay 11-7821
产品介绍
BAY 11-7082 (BAY 11-7821) 是一种IκBα磷酸化和NF-κB抑制剂,选择性且不可逆地抑制 TNF-α 诱导的 IκB-α 磷酸化,并减少 NF-κB 和粘附分子的表达。BAY 11-7082 抑制泛素特异性蛋白酶USP7USP21(IC50分别为 0.19, 0.96 μM)。BAY 11-7082 抑制脂质体中的gasdermin D (GSDMD)孔形成以及炎性体介导的细胞凋亡和人和小鼠细胞中IL-1β的分泌。
生物活性

BAY 11-7082 is anIκBα phosphorylationandNF-κBinhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreasesNF-κBand expression of adhesion molecules. BAY 11-7082 inhibitsubiquitin-specific proteaseUSP7andUSP21(IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibitsgasdermin D (GSDMD)pore formation in liposomes and inflammasome-mediatedpyroptosisand IL-1β secretion in human and mouse cells[1][2][3][4][5].

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[1]. 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[2]. 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[3]. BAY 11-7082 acts by inhibiting TNF-α-induced phosphorylation of IκB-α, resulting in decreased NF-κB and decreases expression of adhesion molecules[4].

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[6].

Animal Model:Four-week-old male BALB/c nude mice with human gastric carcinoma cell lines HGC-27[6]
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.
分子量

207.25

性状

Solid

Formula

C10H9NO2S

CAS 号

19542-67-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(482.51 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.8251 mL24.1255 mL48.2509 mL
5 mM0.9650 mL4.8251 mL9.6502 mL
10 mM0.4825 mL2.4125 mL4.8251 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在本网站选购。