BAY 11-7082

製品コードS2913 バッチS291305

印刷

化学情報

Synonyms

BAY 11-7821

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₀H₉NO₂S

分子量

207.25

CAS No.

19542-67-7

Solubility (25°C)*

体外

DMSO

41 mg/mL (197.82 mM)

Ethanol

3 mg/mL (14.47 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	8.000mg/ml (38.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.000mg/ml (9.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
in vitro	BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. ^[1] This compound (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. It (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. ^[2] This compound (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. This chemical-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. It (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. ^[3] This compound (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. It prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. ^[4] This chemical at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, it at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. It (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. This compound (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of this chemical tested. It (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. ^[5] This compound is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. ^[6]
in vivo	BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.

製品説明

BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.

in vitro

BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. ^[1]

This compound (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. It (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. ^[2]

This compound (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. This chemical-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. It (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. ^[3]

This compound (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. It prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. ^[4]

This chemical at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, it at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. It (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. This compound (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of this chemical tested. It (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. ^[5]

This compound is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. ^[6]

in vivo

BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NCI-H1703 cells
	濃度	~8 μM
	反応時間	12 hours
	実験の流れ	Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [³H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.
動物実験	動物モデル	Male BALB/c nude mice
	投薬量	2.5 & 5 mg/kg
	投与方法	i.t.

参考

https://pubmed.ncbi.nlm.nih.gov/17227230/
https://pubmed.ncbi.nlm.nih.gov/22549160/
https://pubmed.ncbi.nlm.nih.gov/16162000/

https://pubmed.ncbi.nlm.nih.gov/12176906/
https://pubmed.ncbi.nlm.nih.gov/15755516/
https://pubmed.ncbi.nlm.nih.gov/23441730/
https://pubmed.ncbi.nlm.nih.gov/25159004/
https://pubmed.ncbi.nlm.nih.gov/23846545/

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カスタマーフィードバック

: Data from [Data independently produced by Int J Cancer, 2014, 135(2), 282-94]

: Data from [Data independently produced by Cardiovasc Diabetol, 2014, 13, 41]

: Data from [J Biol Chem, 2014, 289(30), 21028-21039]

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NR4A3 potentials M1-like macrophage polarization to facilitate anti-tumor immune responses in breast cancer [ NPJ Breast Cancer, 2025, 11(1):67]	PubMed: 40624019

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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