1. NF-κB
    Cell Cycle/DNA Damage
    Autophagy
    Apoptosis
  2. IKK
    Deubiquitinase
    Autophagy
    Apoptosis
  3. BAY 11-7082

BAY 11-7082 (Synonyms: BAY 11-7821)

目录号: HY-13453 纯度: 99.73%
产品使用指南

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。

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BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure

CAS No. : 19542-67-7

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥650 In-stock
50 mg ¥2200 In-stock
100 mg ¥3000 In-stock
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Customer Review

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

    BAY 11-7082 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Sep;50:30-37.

    BV-2 cells are pretreated with or without Bay11-7082 (10 μM) for 30 min, and then incubated with 20 μM Aβ1–42 for 24 h. The protein expression of TNF-α, IL-1β, and IL-6 are detected by western blot.

    BAY 11-7082 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    Sertoli cells (SC) are pretreated with BAY11-7082 at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium. Expression of p-p65 and MMP-8 is measured by western blotting.

    BAY 11-7082 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2016 Oct;39:149-57.

    AOPPs-induced increase in catabolic factors is regulated by NF-κB activation. Chondrocytes are pretreated with or without NF-κB specific inhibitor Bay11-7082 (0.5 μM), followed by AOPPs treatment. NF-κ B p65 phosphorylation, IκB-α degradation and catabolic factors are detected by Western blot analysis. GAG production is determined by DMB method. Addition of Bay11-7082 blocks AOPPs-induced phosphorylation of NF-κB p65 and prevents degradation of IκB-α.

    BAY 11-7082 purchased from MCE. Usage Cited in: Toxicol Appl Pharmacol. 2017 Mar 22;323:44-52.

    The HUVECs are subjected to NF-κB inhibitor BAY 11-7082 (10 μM) for 1 h prior to MGO (1.0 mM) treatment for 24 h, then Bcl-2/ Bax ratio are determined by western blot.

    BAY 11-7082 purchased from MCE. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975.

    NF-κB-dependent immune responses in testicular cells. Sertoli cells (SC), Leydig cells (LC), and germ cells (GC) are pretreated with BAY11-7082 (BAY) at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium to a final concentration of 1 μM and incubation for 6 h. Expression of phosphorylated NF-κB p65 (p-p65) and total p65 is measured by western blotting. The ratio of p-65/p65 is determined by densitometry and is expressed as means±SEM (n=5).

    BAY 11-7082 purchased from MCE. Usage Cited in: Eur J Med Chem. 2017 Oct 20;139:337-348.

    The cells are treated with different concentrations of compound 6k, and then in the presence or absence of LPS (1 μg/mL) for 24 h. Bay 11-7082 is the NF-κB inhibitors (20 μM). The results are showed as means±SD (n=3) of at least three independent experiments.

    BAY 11-7082 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    BAY 11-7082 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018 Mar 4;19(3):222-229.

    Western blot analysis of PIK3R3, TP, p-P65, P65 expression after transfected with PIK3R3 at the presence of BAY11-7082.

    BAY 11-7082 purchased from MCE. Usage Cited in: Lab Invest. 2018 Apr;98(4):462-476.

    Caco-2BBe cells are pretreated with BAY-11-7082 for 30 min and then treated with TNF-α (100 ng/mL) for 6 h. BAY-11-7082 treatment prevented the TNF-α-induced decrease in downregulated in adenoma (DRA).

    BAY 11-7082 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 1;428:77-89.

    Western blots show that the NF-κB inhibitors BAY11-7082, Parthenolide, and JSH-23 cause dramatic time- and dose-dependent reductions in MGMT protein expression in LN18 and T98G glioma cells.

    BAY 11-7082 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Aug 29;9(9):880.

    NF-κB inhibitor Bay 11-7082 treatment inhibits the activation of SOX4 and EMT process induced by CXCL1.

    BAY 11-7082 purchased from MCE. Usage Cited in: Front Immunol. 2018 Sep 19;9:2121.

    RPMI 2650 cells is incubated with or without IL-17A (100 ng/mL)+BAY 11-7082 (5 μM) for 24 h. WB is performed to measure the expression of MMP-9 protein levels.

    BAY 11-7082 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.

    Real-time PCR analysis shows that meningitic E. coli strains PCN033- and RS218-induced proinflammatory cytokines production is significantly decreased via NF-κB signaling inhibition with 10 μM of BAY11-7082.

    BAY 11-7082 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.

    Real-time PCR analysis shows that meningitic E. coli strains PCN033- and RS218-induced proinflammatory cytokines production is significantly decreased via NF-κB signaling inhibition with 10 μM of BAY11-7082.

    BAY 11-7082 purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Mar;120(3):3898-3910.

    Cells pretreated with SP600125 show a decreased proapoptotic Bax expression and increase antiapoptotic Bcl-2 formation when JNK pathway is blocked. Inhibition of p38 by SB202190 significantly enhanced Bcl-2 expression. Pretreatment with BAY 11-7082 to inhibit NF‐κB markedly enhance Baxm and decrease Bcl-2 expression compared with the ACR-treated group.

    BAY 11-7082 purchased from MCE. Usage Cited in: BMC Cancer. 2019 Jan 8;19(1):30.

    The representative images and analysis of western blot for IκBα、p-IκBα and nuclear p65 in CRC cells and expression levels of E-cadherin, N-cadherin and fibronectin in SW620 and HCT116 cells are measured by western blot treated with BAY 11-7082 (inhibitor of NF-κB pathway).

    BAY 11-7082 purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2019 Jan 13;2019:9406342.

    Protein expressions of AQP3, COX-2 and p-P65 are analyzed by western blot analysis with or without the treatment of BAY and RFP.

    BAY 11-7082 purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2019 Jan 13;2019:9406342.

    The expressions of p-p65, COX-2 and AQP3 are detected by western blotting with or without the treatment of BAY and RFP.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    Description

    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[1][2][3][4][5].

    IC50 & Target[1][2]

    NF-κB

     

    USP7

    0.19 μM (IC50)

    USP21

    0.96 μM (IC50)

    Autophagy

     

    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].

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

    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].

    MCE 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[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.
    Molecular Weight

    207.25

    Formula

    C₁₀H₉NO₂S

    CAS No.

    19542-67-7

    SMILES

    N#C/C=C/S(=O)(C1=CC=C(C)C=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (482.51 mM)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *

    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, 6 months; -20°C, 1 month。-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。

    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 MCE 网站选购。
    References

    Purity: 99.73%

    • 摩尔计算器

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    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    BAY 11-7082BAY 11-7821IKKDeubiquitinaseAutophagyApoptosisIκB kinaseI kappa B kinase DUBsphosphorylationadhesioninflammasomeubiquitinB-celllymphomaleukaemicT-cellcytokineInhibitorinhibitorinhibit

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    产品名称:
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    目录号:
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