BAY 11-7082

別名：BAY 11-7821

製品コード：S2913 純度：99.98%

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.

CAS No. 19542-67-7

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫なし(納期7~10日)
50mg	JPY 55500	国内在庫あり
1g	JPY 298500	国内在庫なし(納期7~10日)

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BAY 11-7082関連製品

関連ターゲット	IκB IKK	もっと見る
関連製品	IKK-16 TPCA-1 Bay 11-7085 BMS-345541 IMD 0354 Bardoxolone Methyl MRT67307 HCl SC-514 LY2409881 TBK1/IKKε-IN-5 PS-1145 Dehydrocostus Lactone Wedelolactone WS6 Mesalazine (5-ASA) BAY-985 AZD3264 WS3 TBK1/IKKε-IN-2 Rosmarinic acid	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Immunology/Inflammation Compound Library Small Molecule Immuno-Oncology Compound Library NF-κB Signaling Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

IκB/IKKシグナル伝達経路

IκB/IKK阻害剤の選択性比較

阻害剤	Citation	IκB	IKK	その他
Resveratrol	68		++	SIRT2,SIRT1,Quinone reductase 2
BAY 11-7082	370	+		E2-conjugating enzymes,USP7,USP21
IKK-16	70		+++
TPCA-1	66		++++	NF-κB,STAT3
BMS-345541	45		++
SC-514	15		+	CDK2/CyclinA,AUR2,PRAK
Bay 11-7085	45	+
MRT67307	2		++++	ULK1
cis-Resveratrol	1		++	SIRT1,Nrf2,PXR
MLN120B	1		+++
TBK1/IKKε-IN-5	6		++++
BAY-985	2		++++	pIRF3
INH14	0		++	NF-κB
Rosmarinic acid	1		+
MRT67307 HCl	18		++++
PS-1145	4		+++
LY2409881	5		+++
IMD 0354	33		✔
Bardoxolone Methyl	33		✔	NF-κB,Ferroptosis,Nrf2
Mesalazine (5-ASA)	4		✔
IMD-0560	0		✔
NF-κB-IN-1	2		✔
Urolithin B	0	✔		skeletal muscle mass,AMPK,Akt
Caulophylline (N-Methylcytisine)	0	✔		NF-κB,MPO,nAChR
Cucurbitacin IIb	0	✔		STAT3,TNF-α,NF-κB
TBK1/IKKε-IN-2	1		✔
Homoplantaginin	0		✔	NF-κB,IL-6,TNF-α
Forsythoside B	0	✔		NF-κB,IL-6,TNF-alpha
Dehydrocostus Lactone	3		✔	COX2
Sarsasapogenin	1	✔		NF-κB,TAK1,IRAK1
AZD3264	1		✔
WS6	3		✔	EBP1
WS3	1		✔	EBP1

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
SP6.5	Growth Inhibition Assay	2.5-20 μM	24 h	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OM431	Function Assay	5 μM	2 h	decreases translocation of p65 in the nucleus	23443086
OCM1	Function Assay	5 μM	2 h	decreases translocation of p65 in the nucleus	23443086
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

E2-conjugating enzymes ^[6] (Cell-free assay)	USP7 ^[7] (Cell-free assay)	USP21 ^[7] (Cell-free assay)	USP6 ^[7] (Cell-free assay)	IκBα phosphorylation ^[1] (Tumor cells)
	0.19 μM	0.96 μM	1.7 μM	10 μM

In Vitro
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] BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. ^[2] Bay 11-7082 (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. Bay 11-7082-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. Bay 11-7082 (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] BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. ^[4] BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (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 BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. ^[5] BAY 11-7082 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]
細胞実験	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.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4 NF-κB p-IKKβ/ IκBα p-IRAK4 / IRAK4		31332209
	Growth inhibition assay	Cell viability Cell viability		31332209

In Vivo
In Vivo	BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.
動物実験	動物モデル	Male BALB/c nude mice
	投与量	2.5 & 5 mg/kg
	投与経路	i.t.

参考
[1] Melisi D, et al. Expert Opin Ther Targets, 2007, 11(2), 133-144. [2] Gastonguay A, et al. Cancer Biol Ther, 2012, 13(8), 647-656. [3] Miwatashi S, et al. J Med Chem, 2005, 48(19), 5966-5979. [4] Mori N, et al. Blood, 2002, 100(5), 1828-1834. [5] Goffi F, et al. Neurosci Lett, 2005, 377(3), 147-151. [6] Strickson S, et al. Biochem J. 2013, 451(3), 427-437. [7] Maria Stella Ritorto, et al. Nat Commun . 2014 Aug 27;5:4763. [8] Chen L, et al. J Gastroenterol. 2014 May;49(5):864-74. + 展開

参考

+ 展開

化学情報

分子量	207.25	化学式	C₁₀H₉NO₂S
CAS No.	19542-67-7	SDF	Download BAY 11-7082 SDFをダウンロードする
Smiles	CC1=CC=C(C=C1)S(=O)(=O)C=CC#N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 41 mg/mL ( (197.82 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 10 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	10%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 45%ddH2O	4.0mg/ml (19.30mM)	Taking the 1 mL working solution as an example, add 100 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 make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	2.0mg/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.
Clear solution	5%DMSO 1 Corn oil	8.0mg/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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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