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

BAY 11-7082  (Synonyms: BAY 11-7821)

目錄號: HY-13453 純度: 99.93%
COA 產(chǎn)品使用指南

BAY 11-7082 (BAY 11-7821) 是一種 IκBα 磷酸化和 NF-κB 抑制劑，選擇性且不可逆地抑制 TNF-α 誘導(dǎo)的 IκB-α 磷酸化，并減少 NF-κB 和粘附分子的表達(dá)。BAY 11-7082 抑制泛素特異性蛋白酶 USP7 和 USP21 (IC50分別為 0.19, 0.96 μM)。BAY 11-7082 抑制脂質(zhì)體中的 gasdermin D (GSDMD) 孔形成以及炎性體介導(dǎo)的細(xì)胞凋亡和人和小鼠細(xì)胞中IL-1β的分泌。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure

CAS No. : 19542-67-7

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2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

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10 mM * 1 mL in DMSO ￥550
In-stock
5 mg ￥500
In-stock
10 mg ￥650
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50 mg ￥2200
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100 mg ￥3000
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 315 篇科研文獻(xiàn)

WB
RT-PCR

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

    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.  [Abstract]

    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 Compl ALlt. 2019 Jan 13;2019:9406342.  [Abstract]

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

    BAY 11-7082 purchased from MCE. Usage Cited in: Evid-Based Compl ALlt. 2019 Jan 13;2019:9406342.  [Abstract]

    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: Cancer Lett. 2018 Aug 1;428:77-89.  [Abstract]

    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: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    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.  [Abstract]

    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: Cell Death Dis. 2018 Aug 29;9(9):880.  [Abstract]

    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: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    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: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    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: Front Immunol. 2018 Sep 19;9:2121.  [Abstract]

    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: Lab Invest. 2018 Apr;98(4):462-476.  [Abstract]

    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 Biol Ther. 2018 Mar 4;19(3):222-229.  [Abstract]

    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: Environ Pollut. 2017 Oct;229:964-975.  [Abstract]

    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.  [Abstract]

    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: Int Immunopharmacol. 2017 Sep;50:30-37.  [Abstract]

    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: Toxicol Appl Pharmacol. 2017 Mar 22;323:44-52.  [Abstract]

    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: Int Immunopharmacol. 2016 Oct;39:149-57.  [Abstract]

    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.

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    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

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

    IC50 & Target[1][2]

    NF-κB

     

    USP7

    0.19 μM (IC50)

    USP21

    0.96 μM (IC50)

    Autophagy

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 IC50
    11 μM
    Compound: BAY-11-7082
    Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay
    Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay
    		[PMID: 32163285]
    HEK293 IC50
    2 μM
    Compound: BAY-11
    Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay
    Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay
    		[PMID: 26343828]
    HEK293 IC50
    2 μM
    Compound: BAY-11
    Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay
    Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay
    		[PMID: 24992702]
    HEK293 IC50
    2 μM
    Compound: BAY-11
    Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay
    Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay
    		[PMID: 24533857]
    HEK293 IC50
    2 μM
    Compound: BAY-11
    Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay
    Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay
    		[PMID: 22850207]
    HEK293 IC50
    2.01 μM
    Compound: BAY-11, BAY-117028
    Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay
    Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay
    		[PMID: 22712432]
    HEK293 IC50
    5 μM
    Compound: BAY-11
    Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay
    Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay
    		[PMID: 23316950]
    RAW264.7 IC50
    1.72 μM
    Compound: BAY11-7082
    Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay
    Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells treated 30 mins before LPS challenge measured after 6 hrs by luciferase reporter gene assay
    		[PMID: 24315191]
    RAW264.7 IC50
    5180 nM
    Compound: BAY11-7082
    Inhibition of LPS stimulated TNF-alpha production in mouse RAW264.7 macrophages preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by EIA
    Inhibition of LPS stimulated TNF-alpha production in mouse RAW264.7 macrophages preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by EIA
    		[PMID: 33601311]
    SH-SY5Y IC50
    0.85 μM
    Compound: Bay 11-7082
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    		[PMID: 36208544]
    SK-N-AS IC50
    1.23 μM
    Compound: Bay 11-7082
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay
    		[PMID: 36208544]
    體外研究
    (In Vitro)

    BAY 11-7082 (BAY 11-7821) 是一種 NF-κB 抑制劑，可誘導(dǎo) HTLV-I 感染的 T 細(xì)胞系凋亡，但僅可忽略 HTLV-I 陰性 T 細(xì)胞的凋亡。Bay 11-7082 快速有效地降低 HTLV-I 感染的 T 細(xì)胞系中 NF-κB 的 DNA 結(jié)合，并下調(diào)受 NF-κB 調(diào)節(jié)的抗凋亡基因 Bcl-xL 的表達(dá)。Bay 11-7082 選擇性抑制人 T 細(xì)胞系中 Tax 誘導(dǎo)的 NF-κB 活性[1]。
    BAY 11-7082 可抑制 NFκB 信號傳導(dǎo)，最近顯示可通過與催化性半胱氨酸殘基共價反應(yīng)來抑制大多數(shù) E2 和 E3 連接酶。此外，BAY 11-7082 還通過與這些酶的催化性 Cys 殘基反應(yīng)來抑制幾種酪氨酸磷酸酶。NSC 697923 最初顯示可抑制 E2 連接酶 Ubc13-Uev1A[2]。
    BAY 11-7082 抑制 IκBα 的磷酸化和 NF-κB 的激活，誘導(dǎo) HBL-1 細(xì)胞死亡。BAY 11-7082 完全抑制 IKKβ 激活環(huán)的 LPS 刺激和 IL-1 刺激磷酸化[3]。
    BAY 11-7082 通過抑制 TNF-α 誘導(dǎo)的 IκB-α 磷酸化，導(dǎo)致 NF-κB 減少和粘附分子表達(dá)減少[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    BAY 11-7082 (2.5 mg/kg 和 5 mg/kg；瘤內(nèi)注射；每周兩次，持續(xù) 21 天) 以劑量依賴性方式顯著抑制腫瘤生長[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.
    分子量

    207.25

    Formula

    C10H9NO2S
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (482.51 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (12.06 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (12.06 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.98%

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.8251 mL 24.1255 mL 48.2509 mL 120.6273 mL
    5 mM 0.9650 mL 4.8251 mL 9.6502 mL 24.1255 mL
    10 mM 0.4825 mL 2.4125 mL 4.8251 mL 12.0627 mL
    15 mM 0.3217 mL 1.6084 mL 3.2167 mL 8.0418 mL
    20 mM 0.2413 mL 1.2063 mL 2.4125 mL 6.0314 mL
    25 mM 0.1930 mL 0.9650 mL 1.9300 mL 4.8251 mL
    30 mM 0.1608 mL 0.8042 mL 1.6084 mL 4.0209 mL
    40 mM 0.1206 mL 0.6031 mL 1.2063 mL 3.0157 mL
    50 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4125 mL
    60 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0105 mL
    80 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5078 mL
    100 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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